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  9 IC50  2 Kd

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 214 hits for monomerid = 185674   

LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 0.75nMAssay Description:Inhibition of human N-terminal his tagged unphosphorylated native ABL1 (229 to 499 residues) expressed in Sf9 cells using ABLtide as substrate preinc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 0.75nMAssay Description:Inhibition of human N-terminal his tagged native ABL1 (229 to 499 residues) expressed in Sf9 cells using ABLtide as substrate preincubated for 2 hrs ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 0.75nMAssay Description:Inhibition of ABL (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of wild type Abl (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/19/2023
Entry Details
PubMed
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of human N-terminal his tagged native ABL1 (229 to 499 residues) expressed in Sf9 cells using ABLtide as substrate preincubated for 2 hrs ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 0.880nMAssay Description:Inhibition of human N-terminal his tagged native ABL1 (229 to 499 residues) expressed in Sf9 cells using ABLtide as substrate preincubated for 2 hrs ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 1.20nMAssay Description:Inhibition of human wild type BLK using PolyEY as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 1.40nMAssay Description:Inhibition of human ABL1 H396P mutant (229 to 499 residues) using ABLtide as substrate preincubated for 2 hrs followed by ATP addition and measured e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetTyrosine-protein kinase Yes(Human)
Frederick National Laboratory For Cancer Research

Curated by ChEMBL
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
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 Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Human)
Ain Shams University

Curated by ChEMBL
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 2nMAssay Description:Inhibition of FLT3 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 2nMAssay Description:Inhibition of human N-terminal his tagged phosphorylated native ABL1 (229 to 499 residues) expressed in Sf9 cells using ABLtide as substrate preincub...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetReceptor-type tyrosine-protein kinase FLT3(Human)
Ain Shams University

Curated by ChEMBL
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 2nMAssay Description:Inhibition of human wild type FLT3 using Poly(Ala,Glu,Lys,Tyr)6:2:5:1 as substrate preincubated for 2 hrs followed by ATP addition and measured every...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetTyrosine-protein kinase Yes(Human)
Frederick National Laboratory For Cancer Research

Curated by ChEMBL
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
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 Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMed
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 4nMAssay Description:Inhibition of human ABL1 T315I mutant (229 to 499 residues) using ABLtide as substrate preincubated for 2 hrs followed by ATP addition and measured e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 4nMAssay Description:Inhibition of human ABL1 T315I mutant (229 to 499 residues) using ABLtide as substrate preincubated for 2 hrs followed by 0.5 mM ATP addition and mea...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 4nMAssay Description:Inhibition of human wild type KDR expressed in Sf9 cells using PolyEY as substrate preincubated for 2 hrs followed by ATP addition and measured every...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 4nMAssay Description:Inhibition of human phosphorylated ABL1 T315I mutant (229 to 499 residues) using ABLtide as substrate preincubated for 2 hrs followed by ATP addition...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 5nMAssay Description:Inhibition of Abl T315I mutant (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/19/2023
Entry Details
PubMed
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 5nMAssay Description:Inhibition of human unphosphorylated ABL1 T315I mutant (229 to 499 residues) using ABLtide as substrate preincubated for 2 hrs followed by ATP additi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 5.5nMAssay Description:Inhibition of human wild type FGFR2 using PolyEY as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 5.5nMAssay Description:Inhibition of human wild type TRKA using PolyEY as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 5.5nMAssay Description:Inhibition of TrkA (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
TargetAngiopoietin-1 receptor(Human)TBA
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 6nMAssay Description:Inhibition of human wild type TIE2 using PolyE4Y as substrate preincubated for 1 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 6.30nMAssay Description:Inhibition of human wild type LCK using PolyEY as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 6.30nMAssay Description:Inhibition of human wild type TAK1 using RB-S6P as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 6.5nMAssay Description:Inhibition of recombinant RIPK1 (unknown origin) by ADP-Glo assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 6.60nMAssay Description:Inhibition of human ABL1 T315I mutant (229 to 499 residues) using ABLtide as substrate preincubated for 2 hrs followed by 5 mM ATP addition and measu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetTyrosine-protein kinase ABL1 [229-512](Human)
Stony Brook University

LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
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
In Depth
Date in BDB:
7/5/2016
Entry Details Article
PubMed
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 7.60nMAssay Description:Inhibition of human wild type MER using PolyEY as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 10nMAssay Description:Inhibition of human wild type FGFR3 using PolyEY as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetMisshapen-like kinase 1(Human)TBA
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 11nMAssay Description:Inhibition of human wild type MINK using RBER-CHKtide as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetProto-oncogene tyrosine-protein kinase Src [251-533](Chicken)
Stony Brook University

LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
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 Depth
Date in BDB:
7/5/2016
Entry Details Article
PubMed
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 12nMAssay Description:Inhibition of human wild type FYN using PolyEY as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 13nMAssay Description:Inhibition of human LYNB preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by spectrophotometric analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 14nMAssay Description:Inhibition of human wild type FGFR1 using PolyEY as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetEphrin type-A receptor 6(Human)TBA
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 17nMAssay Description:Inhibition of human wild type EPHA6 using PolyEY as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 18nMAssay Description:Inhibition of native BCR-ABL T315I mutant autophosphorylation in mouse BaF3 cells incubated for 6 hrs by immunoblot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 19nMAssay Description:Inhibition of human wild type DDR2 using Poly(Ala,Glu,Lys,Tyr)6:2:5:1 as substrate preincubated for 2 hrs followed by ATP addition and measured every...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataEC50:  19nMAssay Description:Inhibition of RCC1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 19nMAssay Description:Inhibition of recombinant RIPK3 (unknown origin) by ADP-Glo assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 25nMAssay Description:Inhibition of human wild type CSK using PolyEY as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 29nMAssay Description:Inhibition of human wild type LYN using PolyEY as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 29nMAssay Description:Inhibition of native BCR-ABL autophosphorylation in mouse BaF3 cells incubated for 6 hrs by immunoblot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetTyrosine-protein kinase Yes(Human)
Frederick National Laboratory For Cancer Research

Curated by ChEMBL
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 33nMAssay Description:Inhibition of human wild type YES using PolyEY as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 34nMAssay Description:Inhibition of human wild type full length SRC (1 to 536 residues) using PolyEY as substrate preincubated for 2 hrs followed by ATP addition and measu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 35nMAssay Description:Inhibition of human wild type MLK1 using RBER-GSK3(14 to 27) as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins f...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 35nMAssay Description:Inhibition of human wild type TRKB using PolyEY as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 37nMAssay Description:Inhibition of human wild type FRK using PolyEY as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 38nMAssay Description:Inhibition of human wild type TRKC using PolyEY as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM185674(Rebastinib | 4-[4-[(5-tert-butyl-2-quinolin-6-ylpy...)
Affinity DataIC50: 38nMAssay Description:Inhibition of human wild type FGR using PolyEY as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
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