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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)

Found 97 hits in this display   

TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataKi:  190nMAssay Description:Binding affinity at hERG expressed in HEK293 cells by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataKi:  280nMAssay Description:Inhibition of recombinant CYP3A4 (unknown origin) expressed in baculosomes in presence of 1 mM NADPHMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataKi:  353nMAssay Description:Displacement of [3H]dofetilide from hERG expressed in HEK293 cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataKi:  2.30E+3nMAssay Description:Time dependent inhibition of CYP3A4More data for this Ligand-Target Pair
TargetVoltage-dependent T-type calcium channel subunit alpha-1H(Homo sapiens (Human))
Icagen

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  32nMAssay Description:Antagonist activity against T-type calcium channel subunit alpha-1H assessed as inactivation of channel current by cell based patch clamp assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  63nMAssay Description:Inhibition of human recombinant CYP2D6-mediated 7-methoxy-4(aminomethyl)-coumarine degradationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  64nMAssay Description:Inhibition of Cav3.1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1I(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  126nMAssay Description:Inhibition of T-type calcium channel alpha1I (unknown origin) by FLIPRMore data for this Ligand-Target Pair
TargetVoltage-dependent T-type calcium channel subunit alpha-1I(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  130nMAssay Description:Inhibition of Cav3.3 (unknown origin)More data for this Ligand-Target Pair
TargetVoltage-dependent T-type calcium channel subunit alpha-1H(Homo sapiens (Human))
Icagen

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  130nMAssay Description:Inhibition of Cav3.2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1H(Homo sapiens (Human))
Icagen

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  130nMAssay Description:Antagonist activity at human alpha1H T-type calcium channel expressed in HEK293 cells by patch clamp techniqueMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  130nMAssay Description:Inhibition of human cytochrome P450 3A4More data for this Ligand-Target Pair
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  156nMAssay Description:Inhibition of voltage-gated L-type Ca channel (species unknown)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1H(Homo sapiens (Human))
Icagen

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  181nMAssay Description:Inhibition of recombinant Cav3.2 channel (unknown origin) expressed in HEK293 cells assessed as effect on calcium flux incubated for 3 mins by FLIPR ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  200nMAssay Description:Inhibition of human Cav3.1 alpha1G expressed in HEK293 cells assessed as inhibition of calcium influx by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent L-type calcium channel subunit alpha-1C(Homo sapiens (Human))
Actelion Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  202nMAssay Description:Inhibition of recombinant Cav1.2 channel (unknown origin) expressed in HEK293 cells assessed as effect on calcium flux incubated for 3 mins by FLIPR ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent L-type calcium channel subunit alpha-1C(Homo sapiens (Human))
Actelion Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  250nMAssay Description:Inhibition of Cav1.2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  300nMAssay Description:Reversible inhibition of CYP3A4More data for this Ligand-Target Pair
TargetVoltage-dependent N-type calcium channel subunit alpha-1B(Homo sapiens (Human))
Icagen

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  416nMAssay Description:Antagonist activity against L-type calcium channel subunit alpha-1C assessed as inactivation of channel current by cell based patch clamp assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM78934(2-methoxyacetic acid [(1S,2S)-2-[2-[3-(1H-benzimid...)
Affinity DataIC50:  470nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using testosterone substrate by LC-MS/MS methodMore data for this Ligand-Target Pair
TargetSodium channel protein type 4 subunit alpha(Rattus norvegicus (Rat))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  500nMAssay Description:Inhibition of rat skeletal muscle Nav1.4 expressed in HEK293 cells by whole cell voltage clamp methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 9 subunit alpha(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  500nMAssay Description:Inhibition of human Nav1.7 expressed in HEK293 cells by whole cell voltage clamp methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  500nMAssay Description:Inhibition of human heart Nav1.5 expressed in HEK293 cells by whole cell voltage clamp methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 2 subunit alpha(Rattus norvegicus)
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  500nMAssay Description:Inhibition of rat brain Nav1.2 expressed in HEK293 cells by whole cell voltage clamp methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  510nMAssay Description:Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunitsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  560nMAssay Description:Inhibition of t-type Cav3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of 50 ms depolarizing voltage step-induced curr...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  560nMAssay Description:Inhibition of T-type CaV3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of calcium current by whole cell patch-clamp me...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  580nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM78934(2-methoxyacetic acid [(1S,2S)-2-[2-[3-(1H-benzimid...)
Affinity DataIC50:  720nMAssay Description:The CYP3A4 inhibition assays were conducted using Human Liver Microsomes purchased from Invitrogen and designed to screen potential inhibitors of Cyt...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCytochrome P450 3A4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM78934(2-methoxyacetic acid [(1S,2S)-2-[2-[3-(1H-benzimid...)
Affinity DataIC50:  720nMAssay Description:The CYP2D6 inhibition assays were conducted using Human Liver Microsomes purchased from Invitrogen and designed to screen potential inhibitors of Cyt...More data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  806nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  830nMAssay Description:Inhibition of T-type CaV3.1 channel expressed in HEK293 cells assessed as inhibition of calcium current by automated patch-clamp assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  830nMAssay Description:Inhibition of alpha-1G calcium channel in human HEK293 cells by whole-cell patch-clamp methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  840nMAssay Description:Concentration of the compounds required for inhibition of HEK293 cells (alpha1G T-type)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  840nMAssay Description:Inhibition of alpha1G T-type calcium channel expressed in HEK293 cells by electrophysiological methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM78934(2-methoxyacetic acid [(1S,2S)-2-[2-[3-(1H-benzimid...)
Affinity DataIC50:  840nMAssay Description:Inhibition of CYP2D6 in human liver microsomes using bufuralol substrate by LC-MS/MS methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  860nMAssay Description:Inhibition of T-type CaV3.1 channel expressed in HEK293 cells assessed as inhibition of calcium current by manual patch-clamp assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 7 subunit alpha(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  980nMAssay Description:Inhibition of Na channel (species unknown)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1I(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.00E+3nMAssay Description:Inhibition of T-type Cav3.3 channelMore data for this Ligand-Target Pair
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.00E+3nMAssay Description:Inhibition of rat Cav2.2-alpha1beta/beta3 expressed in HEK293 cells assessed as decrease in calcium mobilization response to KCl after 1 hr by Fluo-4...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1H(Homo sapiens (Human))
Icagen

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.00E+3nMAssay Description:Inhibition of human T-type calcium channel Cav3.2 expressed in T-Rex293 cells by whole cell patch clamp assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1H(Homo sapiens (Human))
Icagen

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.00E+3nMAssay Description:Inhibition of T-type Cav3.2 channelMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.00E+3nMAssay Description:Inhibition of T-type Cav3.1 channelMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-dependent translocase ABCB1(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.20E+3nMAssay Description:TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.30E+3nMAssay Description:Inhibition of human ERG expressed in HEK cells by patch clamp assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C19(Homo sapiens (Human))
Tongji University

Curated by ChEMBL
LigandPNGBDBM78934(2-methoxyacetic acid [(1S,2S)-2-[2-[3-(1H-benzimid...)
Affinity DataIC50:  1.32E+3nMAssay Description:Inhibition of CYP2C19 in human liver microsomes using omeprazole substrate by LC-MS/MS methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.34E+3nMAssay Description:Ability to block calcium channel T type 3.1v expressed in HEK293 cells by whole cell patch clamp methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.34E+3nMAssay Description:Inhibition of human Cav3.1 expressed in tsA-201 cells by patch clamp electrophysiologyMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.34E+3nMAssay Description:Inhibition of T type calcium channel Cav3.1 (unknown origin) expressed in HEK293T cells by patch clamp method relative to controlMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.34E+3nMAssay Description:Inhibition of T-type alpha1G calcium channel expressed in HEK293 cells assessed as Kcl-induced depolarizaionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.34E+3nMAssay Description:Inhibition of T type calcium channel subunit alpha1G expressed in HEK293 cells assessed as effect on T-type calcium currents by patch clamp methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.34E+3nMAssay Description:Inhibition of human ERG by patch clamp assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.34E+3nMAssay Description:Inhibition of T-type calcium channel Cav3.1 alpha1G subunit expressed in HEK293 cells assessed as calcium current by patch-clamp assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.34E+3nMAssay Description:Inhibition of T-type [Ca2+] channel (alpha1G) expressed in HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.34E+3nMAssay Description:Inhibition of T-type calcium channel Cav3.1 expressed in HEK293 cells co-expressing alpha1G subunit and Kir2.1 potassium channel by patch-clamp assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.34E+3nMAssay Description:Inhibition of human ERG by whole-cell patch clamp methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent N-type calcium channel subunit alpha-1B(Homo sapiens (Human))
Icagen

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.34E+3nMAssay Description:Inhibition of N-type calcium channel alpha1BMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.34E+3nMAssay Description:Inhibition of T-type alpha1G channel expressed in HEK293 cells by whole-cell patch-clamp methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.34E+3nMAssay Description:Antagonist activity at T type calcium channel alpha1G (unknown origin) expressed in HEK293 cells assessed as inhibition of peak currents by whole-cel...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.34E+3nMAssay Description:Inhibition of T-type calcium channel Cav3.1 expressed in HEK293 cells coexpressing alpha1G subunit by whole-cell patch clamp methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.34E+3nMAssay Description:Inhibition of T-type calcium channel alpha1G expressed in human HEK293 cells assessed as inhibition of peak currents by whole-cell patch-clamp methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.40E+3nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.40E+3nMAssay Description:Inhibitory concentration against IKr potassium channelMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.40E+3nMAssay Description:Inhibition of human hERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.40E+3nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.43E+3nMAssay Description:K+ channel blocking activity in COS-7 African green monkey kidney derived cells expressing HERG Kv11.1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent T-type calcium channel subunit alpha-1G(Homo sapiens (Human))
Idorsia Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.43E+3nMAssay Description:Inhibition of T-type calcium channel Cav3.1 with alpha1G subunit by patch clamp assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.45E+3nMAssay Description:Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open stateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.45E+3nMAssay Description:Inhibition of human Potassium channel HERG expressed in mammalian cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.45E+3nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.45E+3nMAssay Description:Inhibition of human ERG in MCF7 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.45E+3nMAssay Description:Inhibitory concentration against potassium channel HERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.45E+3nMAssay Description:Inhibition of human ERG expressed in CHO cells by whole cell patch clamp techniqueMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-dependent translocase ABCB1(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.50E+3nMAssay Description:Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCECMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-dependent translocase ABCB1(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.60E+3nMAssay Description:TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cellsMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetATP-dependent translocase ABCB1(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.80E+3nMAssay Description:Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-dependent translocase ABCB1(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.80E+3nMAssay Description:TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.80E+3nMAssay Description:Inhibition of hERG K channelMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2J2(Homo sapiens (Human))
Tongji University

Curated by ChEMBL
LigandPNGBDBM78934(2-methoxyacetic acid [(1S,2S)-2-[2-[3-(1H-benzimid...)
Affinity DataIC50:  2.14E+3nMAssay Description:Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  3.30E+3nMAssay Description:Inhibition of human ERG expressed in CHO cells by IONWORKS assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-dependent translocase ABCB1(Mus musculus (Mouse))
F. Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  7.40E+3nMAssay Description:Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-dependent translocase ABCB1(Mus musculus)
F. Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.00E+4nMAssay Description:Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUbiquitin-conjugating enzyme E2 N(Homo sapiens (Human))
Burnham Center For Chemical Genomics

Curated by PubChem BioAssay
LigandPNGBDBM78934(2-methoxyacetic acid [(1S,2S)-2-[2-[3-(1H-benzimid...)
Affinity DataIC50: >2.00E+4nMAssay Description:Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG) Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego CA...More data for this Ligand-Target Pair
In DepthDetails PCBioAssay
TargetPotassium channel subfamily K member 9(Homo sapiens (Human))
Universidad De Talca

Curated by ChEMBL
LigandPNGBDBM78934(2-methoxyacetic acid [(1S,2S)-2-[2-[3-(1H-benzimid...)
Affinity DataIC50:  2.46E+4nMAssay Description:Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM78934(2-methoxyacetic acid [(1S,2S)-2-[2-[3-(1H-benzimid...)
Affinity DataIC50:  2.50E+4nMAssay Description:Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate t...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C9(Homo sapiens (Human))
Tongji University

Curated by ChEMBL
LigandPNGBDBM78934(2-methoxyacetic acid [(1S,2S)-2-[2-[3-(1H-benzimid...)
Affinity DataIC50:  2.84E+4nMAssay Description:Inhibition of CYP2C9 in human liver microsomes using tolbutamide substrate by LC-MS/MS methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM78934(2-methoxyacetic acid [(1S,2S)-2-[2-[3-(1H-benzimid...)
Affinity DataIC50:  4.38E+4nMAssay Description:Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 1A2(Homo sapiens (Human))
Tongji University

Curated by ChEMBL
LigandPNGBDBM78934(2-methoxyacetic acid [(1S,2S)-2-[2-[3-(1H-benzimid...)
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of CYP1A2 in human liver microsomes using phenacetin substrate by LC-MS/MS methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCalcium release-activated calcium channel protein 1(Homo sapiens (Human))
The University Of Queensland

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  5.21E+4nMAssay Description:Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction of SERCA inhibition-induced ER release preincu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCalcium release-activated calcium channel protein 1(Homo sapiens (Human))
The University Of Queensland

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction in BAPTA-induced Ca2+ depletion-stimulated SOC...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVoltage-dependent L-type calcium channel subunit alpha-1C(Homo sapiens (Human))
Actelion Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM78934(2-methoxyacetic acid [(1S,2S)-2-[2-[3-(1H-benzimid...)
Affinity DataIC50:  1.08E+5nMAssay Description:Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunitMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM78934(2-methoxyacetic acid [(1S,2S)-2-[2-[3-(1H-benzimid...)
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM78934(2-methoxyacetic acid [(1S,2S)-2-[2-[3-(1H-benzimid...)
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 2(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM78934(2-methoxyacetic acid [(1S,2S)-2-[2-[3-(1H-benzimid...)
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataIC50:  1.40E+5nMAssay Description:Time dependent inhibition of CYP3A4 in human liver microsomes assessed as reduction in testosterone 6beta-hydroxylation incubated for 60 mins in pres...More data for this Ligand-Target Pair
TargetVoltage-dependent L-type calcium channel subunit alpha-1C(Homo sapiens (Human))
Actelion Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM78934(2-methoxyacetic acid [(1S,2S)-2-[2-[3-(1H-benzimid...)
Affinity DataIC50:  2.88E+5nMAssay Description:Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Xenopus oocyte heterologically expressing alpha-1C subunitMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium channel subfamily K member 2(Homo sapiens (Human))
Korea Institute of Science and Technology

LigandPNGBDBM50117922((1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl)...)
Affinity DataEC50:  500nMpH: 7.3 T: 2°CAssay Description:The hTREK1 stable cell lines were seeded at a density of 10 000 cells/well in a 12-well plate. Whole-cell membrane currents were amplified using the ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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