Compile Data Set for Download or QSAR
Report error Found 86 Enz. Inhib. hit(s) with all data for entry = 50042476
TargetP2X purinoceptor 7(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50426571(CHEMBL2324343)
Affinity DataIC50: 0.0100nMAssay Description:Inhibition of P2X7 receptor (unknown origin) assessed as inhibition of IL1beta productionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50066789(A-85380,5-Iodo | CHEMBL123433 | A-85380-I | 3-((S)...)
Affinity DataKi:  0.0500nMAssay Description:Displacement of [3H]epibatidine from alpha4beta2 nAChR in rat brain membraneMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50166908(CHEMBL556954 | VARENICLINE | 5,8,14-triazatetracyc...)
Affinity DataKi:  0.0600nMAssay Description:Binding affinity to alpha4beta2 nAChR in rat cortexMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM26263(ethyl 12-fluoro-8-methyl-9-oxo-2,4,8-triazatricycl...)
Affinity DataKd:  0.450nMAssay Description:Binding affinity to human GABAA alpha3beta2gamma2 expressed in thymidine kinase-deficient L cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50067424((S)-9-Methoxy-7-oxo-3b,4,5,6-tetrahydro-7H-2,6a,11...)
Affinity DataKi:  0.450nMAssay Description:Positive allosteric modulation of GABAA alpha5 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50142570(9-(4-Methyl-thiazol-2-yl)-11-pyridin-4-yl-6,7-dihy...)
Affinity DataKi:  0.5nMAssay Description:Positive allosteric modulation of GABAA alpha3 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50142570(9-(4-Methyl-thiazol-2-yl)-11-pyridin-4-yl-6,7-dihy...)
Affinity DataKi:  0.600nMAssay Description:Positive allosteric modulation of GABAA alpha2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50179998(7-tert-butyl-3-(2,5-difluorophenyl)-6-((2-methyl-2...)
Affinity DataKi:  0.700nMAssay Description:Positive allosteric modulation of GABAA alpha3 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50179998(7-tert-butyl-3-(2,5-difluorophenyl)-6-((2-methyl-2...)
Affinity DataKi:  0.700nMAssay Description:Positive allosteric modulation of GABAA alpha2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50156083(3-tert-Butyl-7-(5-methyl-isoxazol-3-yl)-2-(2-methy...)
Affinity DataKi:  0.800nMAssay Description:Positive allosteric modulation of GABAA alpha1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50156083(3-tert-Butyl-7-(5-methyl-isoxazol-3-yl)-2-(2-methy...)
Affinity DataKi:  0.800nMAssay Description:Positive allosteric modulation of GABAA alpha3 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50156083(3-tert-Butyl-7-(5-methyl-isoxazol-3-yl)-2-(2-methy...)
Affinity DataKi:  0.800nMAssay Description:Positive allosteric modulation of GABAA alpha2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50142570(9-(4-Methyl-thiazol-2-yl)-11-pyridin-4-yl-6,7-dihy...)
Affinity DataKi:  1.30nMAssay Description:Positive allosteric modulation of GABAA alpha1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50156083(3-tert-Butyl-7-(5-methyl-isoxazol-3-yl)-2-(2-methy...)
Affinity DataKi:  1.40nMAssay Description:Positive allosteric modulation of GABAA alpha5 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50179998(7-tert-butyl-3-(2,5-difluorophenyl)-6-((2-methyl-2...)
Affinity DataKi:  2.30nMAssay Description:Positive allosteric modulation of GABAA alpha5 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50426573(CHEMBL2324349 | US9434711, 306)
Affinity DataIC50: 4nMAssay Description:Inhibition of TRPM8 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50331290(N-(3-aminopropyl)-2-(3-methylbenzyloxy)-N-(thiophe...)
Affinity DataIC50: 4nMAssay Description:Inhibition of TRPM8 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50371391(SENICAPOC)
Affinity DataIC50: 6nMAssay Description:Inhibition of Kca 3.1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetGABA-A receptor; alpha-5/beta-3/gamma-2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50000766(CHEMBL12 | DIAZEPAM | US9271961, Diazepam)
Affinity DataIC50: 17nMAssay Description:Binding affinity to human recombinant GABAA alpha5beta3gamma2 expressed in Xenopus laevis oocytes by patch clamp techniqueMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50426576(CHEMBL2324346)
Affinity DataEC50:  20nMAssay Description:Inhibition of human Kca 2.3 expressed in HEK293 cells by patch clamp techniqueMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetP2X purinoceptor 3(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50426572(CHEMBL2324342)
Affinity DataIC50: 21nMAssay Description:Antagonist activity at human P2X3 expressed in rat liver endothelium cells assessed as inhibition of the intracellular calcium increase after 30 to 4...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetP2X purinoceptor 3(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50379716(CHEMBL2011125)
Affinity DataIC50: 24nMAssay Description:Antagonist activity at human P2X3 expressed in rat liver endothelium cells assessed as inhibition of the intracellular calcium increase after 30 to 4...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50067424((S)-9-Methoxy-7-oxo-3b,4,5,6-tetrahydro-7H-2,6a,11...)
Affinity DataKi:  25nMAssay Description:Positive allosteric modulation of GABAA alpha3 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50067424((S)-9-Methoxy-7-oxo-3b,4,5,6-tetrahydro-7H-2,6a,11...)
Affinity DataKi:  27nMAssay Description:Positive allosteric modulation of GABAA alpha2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50330932(N-((2-Morpholin-4-yl-pyridin-3-yl)methyl)-6-(4-cya...)
Affinity DataIC50: 30nMAssay Description:Inhibition of voltage-gated Na channel 1.8 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50344821(10-hydroxymethyl-5-imino-(2S)-12,13-dioxa-4,6-diaz...)
Affinity DataIC50: 30nMAssay Description:Inhibition of voltage-gated Na channel 1.2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50426577(CHEMBL2324354)
Affinity DataIC50: 30nMAssay Description:Inhibition of human voltage-gated Na channel 1.3More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50344821(10-hydroxymethyl-5-imino-(2S)-12,13-dioxa-4,6-diaz...)
Affinity DataIC50: 30nMAssay Description:Inhibition of voltage-gated Na channel 1.8 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50344821(10-hydroxymethyl-5-imino-(2S)-12,13-dioxa-4,6-diaz...)
Affinity DataIC50: 30nMAssay Description:Inhibition of voltage-gated Na channel 1.6 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50344821(10-hydroxymethyl-5-imino-(2S)-12,13-dioxa-4,6-diaz...)
Affinity DataIC50: 30nMAssay Description:Inhibition of voltage-gated Na channel 1.3 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50344821(10-hydroxymethyl-5-imino-(2S)-12,13-dioxa-4,6-diaz...)
Affinity DataIC50: 30nMAssay Description:Inhibition of voltage-gated Na channel 1.5 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50344821(10-hydroxymethyl-5-imino-(2S)-12,13-dioxa-4,6-diaz...)
Affinity DataIC50: 30nMAssay Description:Inhibition of voltage-gated Na channel 1.4 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50344821(10-hydroxymethyl-5-imino-(2S)-12,13-dioxa-4,6-diaz...)
Affinity DataIC50: 30nMAssay Description:Inhibition of voltage-gated Na channel 1.7 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50344821(10-hydroxymethyl-5-imino-(2S)-12,13-dioxa-4,6-diaz...)
Affinity DataIC50: 30nMAssay Description:Inhibition of voltage-gated Na channel 1.9 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50344821(10-hydroxymethyl-5-imino-(2S)-12,13-dioxa-4,6-diaz...)
Affinity DataIC50: 30nMAssay Description:Inhibition of voltage-gated Na channel 1.1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetPotassium channel subfamily K member 9(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50426570(CHEMBL2324344)
Affinity DataIC50: 35nMAssay Description:Inhibition of TASK-3 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50067424((S)-9-Methoxy-7-oxo-3b,4,5,6-tetrahydro-7H-2,6a,11...)
Affinity DataKi:  49nMAssay Description:Positive allosteric modulation of GABAA alpha1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50390072(CHEMBL2069427)
Affinity DataIC50: 66nMAssay Description:Inhibition of human voltage-gated Na channel 1.7 by cell based patch clamp techniqueMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50426578(CHEMBL2324352)
Affinity DataIC50: 90nMAssay Description:Inhibition of human voltage-gated Na channel 1.7 expressed in HEK293 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50004798(CHEMBL2324356)
Affinity DataIC50: 100nMAssay Description:Inhibition of voltage-gated K channel 2.2 (unknown origin) by automated patch clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50126761(2-Amino-3-(5-tert-butyl-3-hydroxy-isothiazol-4-yl)...)
Affinity DataEC50:  100nMAssay Description:Agonist activity at GluK1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50170602([(E)-(S)-4-(5-Isopropoxy-pyridin-3-yl)-1-methyl-bu...)
Affinity DataEC50:  106nMAssay Description:Agonist activity at human alpha4beta2 nAChR expressed in HEK293 cells incubated for 5 mins measured every second for 1 mins followed by every 5 secs ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50300204((R)-N-benzyl 2-acetamido-3-methoxypropionamide, | ...)
Affinity DataIC50: 182nMAssay Description:Binding affinity to human inactivated voltage-gated Na channel 1.7 expressed in HEK293 cells by patch-clamp techniqueMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM86521(CAS_5719 | NSC_5719 | Zaleplon)
Affinity DataEC50:  290nMAssay Description:Modulation of human GABA-A alpha1beta2gamma2 expressed in xenopus oocytes assessed as potentiation of GABA-evoked chloride currentsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetPotassium channel subfamily K member 3(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50426570(CHEMBL2324344)
Affinity DataIC50: 300nMAssay Description:Inhibition of TASK-1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50426567(BMS-204352 | MaxiPost | FLINDOKALNER)
Affinity DataEC50:  352nMAssay Description:Positive modulation of Kca 1.1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetPotassium channel subfamily K member 2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM79180(MLS001331726 | cid_60496 | benzenesulfonic acid;3-...)
Affinity DataIC50: 400nMAssay Description:Inhibition of TREK-1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50300204((R)-N-benzyl 2-acetamido-3-methoxypropionamide, | ...)
Affinity DataIC50: 415nMAssay Description:Binding affinity to rat inactivated voltage-gated Na channel 1.3 expressed in human HEK293 cells by patch-clamp techniqueMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM86751(CHEMBL14935 | LY-293558 | LY 293558)
Affinity DataIC50: 500nMAssay Description:Inhibition of GluK1 receptor (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50426578(CHEMBL2324352)
Affinity DataIC50: 680nMAssay Description:Inhibition of human voltage-gated Na channel 1.8 expressed in HEK293 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
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