BDBM185674 4-[4-[(5-tert-butyl-2-quinolin-6-ylpyrazol-3-yl)carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide::Rebastinib

SMILES CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3cc(nn3-c3ccc4ncccc4c3)C(C)(C)C)c(F)c2)ccn1

InChI Key InChIKey=WVXNSAVVKYZVOE-UHFFFAOYSA-N

Data  7 IC50  2 Kd

PDB links: 6 PDB IDs match this monomer.

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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 9 hits for monomerid = 185674   

TargetTyrosine-protein kinase ABL1 [229-512](Homo sapiens (Human))
Stony Brook University

LigandPNGBDBM185674(4-[4-[(5-tert-butyl-2-quinolin-6-ylpyrazol-3-yl)ca...)
Affinity DataKd:  7.20nMAssay Description:Inhibitor selectivity profiles were obtained through Luceome Biotechnologies (Tuscon, AZ). Each inhibitor was screened at 0.5 μM against a panel...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase Src [251-533](Gallus gallus (Chicken))
Stony Brook University

LigandPNGBDBM185674(4-[4-[(5-tert-butyl-2-quinolin-6-ylpyrazol-3-yl)ca...)
Affinity DataKd:  11nMAssay Description:Inhibitor selectivity profiles were obtained through Luceome Biotechnologies (Tuscon, AZ). Each inhibitor was screened at 0.5 μM against phospho...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Yes(Homo sapiens (Human))
Frederick National Laboratory For Cancer Research

Curated by ChEMBL
LigandPNGBDBM185674(4-[4-[(5-tert-butyl-2-quinolin-6-ylpyrazol-3-yl)ca...)
Affinity DataIC50:  2.5nMAssay Description:Inhibition of Yes1 (unknown origin) assessed as kinase-dependent enzymatic production of ADP from ATP using coupled luminescence-based reaction by AD...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase Yes(Homo sapiens (Human))
Frederick National Laboratory For Cancer Research

Curated by ChEMBL
LigandPNGBDBM185674(4-[4-[(5-tert-butyl-2-quinolin-6-ylpyrazol-3-yl)ca...)
Affinity DataIC50:  1.5nMAssay Description:Inhibition of Yes1 (unknown origin) by [gamma-33P]-ATP radiolabeled enzyme activity assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ABL1(Homo sapiens (Human))
Hangzhou Medical College

Curated by ChEMBL
LigandPNGBDBM185674(4-[4-[(5-tert-butyl-2-quinolin-6-ylpyrazol-3-yl)ca...)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of wild type Abl (unknown origin)More data for this Ligand-Target Pair
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Ain Shams University

Curated by ChEMBL
LigandPNGBDBM185674(4-[4-[(5-tert-butyl-2-quinolin-6-ylpyrazol-3-yl)ca...)
Affinity DataIC50:  5.5nMAssay Description:Inhibition of TrkA (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetTyrosine-protein kinase ABL1(Homo sapiens (Human))
Hangzhou Medical College

Curated by ChEMBL
LigandPNGBDBM185674(4-[4-[(5-tert-butyl-2-quinolin-6-ylpyrazol-3-yl)ca...)
Affinity DataIC50:  0.75nMAssay Description:Inhibition of ABL (unknown origin)More data for this Ligand-Target Pair
TargetTyrosine-protein kinase ABL1(Homo sapiens (Human))
Hangzhou Medical College

Curated by ChEMBL
LigandPNGBDBM185674(4-[4-[(5-tert-butyl-2-quinolin-6-ylpyrazol-3-yl)ca...)
Affinity DataIC50:  5nMAssay Description:Inhibition of Abl T315I mutant (unknown origin)More data for this Ligand-Target Pair
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
Ain Shams University

Curated by ChEMBL
LigandPNGBDBM185674(4-[4-[(5-tert-butyl-2-quinolin-6-ylpyrazol-3-yl)ca...)
Affinity DataIC50:  2nMAssay Description:Inhibition of FLT3 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed