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

Found 40 hits in this display   

TargetProto-oncogene tyrosine-protein kinase ROS(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataKi:  2.00E+3nMAssay Description:Inhibition of ROS1 L2026M mutant (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProto-oncogene tyrosine-protein kinase ROS(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataKi:  2.40E+3nMAssay Description:Inhibition of wild type ROS1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProto-oncogene tyrosine-protein kinase ROS(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataKi: >3.00E+3nMAssay Description:Inhibition of ROS1 G2032R mutant (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  0.590nMAssay Description:Inhibition of N-terminal GST tagged wild-type human ALK cytoplasmic domain (1058-1620 amino acids) expressed Sf9 cells pre-incubated for 30 mins befo...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  0.960nMAssay Description:Inhibition of human ALK S1206Y mutant expressed Sf9 cells pre-incubated for 30 mins before addition of Ulight-CKKSRGDYMTMQIG substrate and measured a...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  1.5nMAssay Description:Inhibition of human ALK L1196M mutant expressed Sf9 cells pre-incubated for 30 mins before addition of Ulight-CKKSRGDYMTMQIG substrate and measured a...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of ALK L1196M (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of ALK (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of ALK (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of ALK (unknown origin)More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  1.90nMAssay Description:Inhibition of ALK using Bio-Gastrintide as substrate by TR-FRET assay in presence of 30 uM of ATPMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor/Echinoderm microtubule-associated protein-like 4(Homo sapiens (Human))
Dana-Farber Cancer Institute

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  2nMAssay Description:Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assayMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  2.10nMAssay Description:Inhibition of ALK G1202R (unknown origin)More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  3.90nMAssay Description:Inhibition of human ALK G1269A mutant expressed Sf9 cells pre-incubated for 30 mins before addition of Ulight-CKKSRGDYMTMQIG substrate and measured a...More data for this Ligand-Target Pair
TargetStromelysin-3(Mus musculus)
University Of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  4.5nMAssay Description:Antiproliferative activity against human NB1 cells harbouring ALK by CellTiter-Glo luminescent cell viability assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetALK tyrosine kinase receptor/Echinoderm microtubule-associated protein-like 4(Homo sapiens (Human))
Dana-Farber Cancer Institute

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  4.5nMAssay Description:Inhibition of EML4/ALK in human NCI-H2228 cellsMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  4.80nMAssay Description:Inhibition of wild type recombinant human RET using Biotin-EGPWLEEEEEAYGWMDF as substrate incubated for 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  4.80nMAssay Description:Inhibition of human recombinant RET using Biotin-EGPWLEEEEEAYGWMDFas substrate by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  5.30nMAssay Description:ALK-inhibiting activity was measured by following an activity of inhibiting phosphorylation by biotinylated peptide (EGPWLEEEEEAYGWMDF). For the dete...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  5.70nMAssay Description:Inhibition of human recombinant RET M918T using Biotin-EGPWLEEEEEAYGWMDF as substrate by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  8.30nMAssay Description:Inhibition of human recombinant RET S891A using Biotin-EGPWLEEEEEAYGWMDF as substrate by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  9.5nMAssay Description:Inhibition of human recombinant RET G691S using Biotin-EGPWLEEEEEAYGWMDF as substrate by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetCyclin-G-associated kinase(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50: <10nMAssay Description:Inhibition of human GAKMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSRSF protein kinase 1(Homo sapiens (Human))
Dana-Farber Cancer Institute

US Patent
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  11nMAssay Description:SRPK1 Inhibitory Activities of the Compounds.More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  12nMAssay Description:Inhibition of recombinant ALK (unknown origin) using poly (Glu, Tyr)4:1 substrate incubated for 60 mins by ELISAMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  15nMAssay Description:Inhibition of gatekeeper ALK L1196M mutant (unknown origin) using poly (Glu, Tyr)4:1 substrate incubated for 60 mins by ELISAMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  19nMAssay Description:Inhibition of ALK expressed in human NCI-H3122 cells assessed as cell growth inhibition after 72 hrs by SRB/CCK-8 assayMore data for this Ligand-Target Pair
TargetSRSF protein kinase 2(Homo sapiens (Human))
Dana-Farber Cancer Institute

US Patent
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  28.2nMAssay Description:SRPK1 Inhibitory Activities of the Compounds.More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  32nMAssay Description:Inhibition of human recombinant RET V804L using Biotin-EGPWLEEEEEAYGWMDF as substrate by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  52nMAssay Description:A reaction buffer (100 mM HEPES (pH 7.4), 10 mM MgCl2, 0.003% Brij-35, 0.004% Tween-20, and 1 mM DTT) was mixed with a RET recombinant protein (RET—w...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  53nMAssay Description:Inhibition of human recombinant RET V804M using Biotin-EGPWLEEEEEAYGWMDF as substrate by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetSRSF protein kinase 1(Homo sapiens (Human))
Dana-Farber Cancer Institute

US Patent
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  195nMAssay Description:Inhibition of SRPK1 (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804L](Homo sapiens (Human))
Daiichi Sankyo

US Patent
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  811nMAssay Description:A reaction buffer (100 mM HEPES (pH 7.4), 10 mM MgCl2, 0.003% Brij-35, 0.004% Tween-20, and 1 mM DTT) was mixed with a RET recombinant protein (RET—w...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  1.03E+3nMAssay Description:Binding affinity to ALK (unknown origin) using TK as substrate incubated for 1 hr in presence of ATP by HTRF analysisMore data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Zhejiang University

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  1.40E+3nMAssay Description:Inhibition of KDR (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Zhejiang University

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  1.40E+3nMAssay Description:Inhibition of KDR using Bio-Gastrintide as substrate by TR-FRET assay in presence of 50 uM of ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBroad substrate specificity ATP-binding cassette transporter ABCG2(Homo sapiens (Human))
Federal University Of Parana

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50:  1.50E+3nMAssay Description:Inhibition of ABCG2 (unknown origin) expressed in human HEK293 cells mediated efflux by flow cytometryMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetHepatocyte growth factor receptor(Homo sapiens (Human))
Chugai Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50: >5.00E+3nMAssay Description:Inhibition of MET using Bio-HER2tide as substrate by TR-FRET assay in presence of 50 uM of ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMast/stem cell growth factor receptor Kit(Homo sapiens (Human))
Chugai Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50: >5.00E+3nMAssay Description:Inhibition of KIT using Bio-HER2tide as substrate by TR-FRET assay in presence of 50 uM of ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Ocean University Of China

Curated by ChEMBL
LigandPNGBDBM50362781(1256580-46-7 | AF802 | Alecensa | Alectinib | CH54...)
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed