BDBM50299148 (S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrrolo[1,2-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide::1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl}-N-(6-fluoropyridin-3-yl)-2-methyl-L-prolinamide::BMS-754807::CHEMBL575448

SMILES C[C@]1(CCCN1c1nc(Nc2cc([nH]n2)C2CC2)c2cccn2n1)C(=O)Nc1ccc(F)nc1

InChI Key InChIKey=LQVXSNNAFNGRAH-UHFFFAOYSA-N

Data  21 IC50  1 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 106 hits for monomerid = 50299148   

TargetInsulin receptor(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 1.70nMAssay Description:Inhibition of IR (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMed
TargetInsulin receptor(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 1.70nMAssay Description:Inhibition of recombinant IR (unknown origin) incubated for 60 mins in presence of ATP by electrophoretic caliper fluorescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetInsulin-like growth factor 1 receptor(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 1.80nMAssay Description:Inhibition of IGF-1R (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMed
TargetInsulin-like growth factor 1 receptor(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 1.80nMAssay Description:Inhibition of recombinant human IGF-1R using KKSRGDYMTMQIG as substrate incubated for 60 mins in presence of ATP by electrophoretic caliper fluoresce...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetInsulin-like growth factor 1 receptor(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 2nMAssay Description:Inhibition of IGF1R after 60 mins by fluorescence electrophoresisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/26/2012
Entry Details Article
PubMed
TargetInsulin-like growth factor 1 receptor(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 2.10nMAssay Description:Inhibition of IGF1R in IGF1R-SAL cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
TargetBDNF/NT-3 growth factors receptor(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 4nMAssay Description:Inhibition of TRKB (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMed
TargetBDNF/NT-3 growth factors receptor(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 4.10nMAssay Description:Inhibition of recombinant TrkB (unknown origin) incubated for 60 mins in presence of ATP by electrophoretic caliper fluorescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 5.60nMAssay Description:Inhibition of recombinant Met (unknown origin) incubated for 60 mins in presence of ATP by electrophoretic caliper fluorescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetInsulin-like growth factor 1 receptor(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 6nMAssay Description:Inhibition of IGF-1R phosphorylation in human Rh41 cells at 0.1 to 1000 nmol/L incubated for 1 hr by Western blotting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetHigh affinity nerve growth factor receptor(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 7nMAssay Description:Inhibition of TRKA (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 7.40nMAssay Description:Inhibition of recombinant TrkA (unknown origin) incubated for 60 mins in presence of ATP by electrophoretic caliper fluorescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetInsulin-like growth factor 1 receptor(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 8.40nMAssay Description:Inhibition of IGF1RMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2011
Entry Details Article
PubMed
TargetAurora kinase A(Human)TBA
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 9nMAssay Description:Inhibition of recombinant AurA (unknown origin) incubated for 60 mins in presence of ATP by electrophoretic caliper fluorescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetInsulin-like growth factor 1 receptor(Mouse)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 13nMAssay Description:Inhibition of IGF1R phosphorylation in mouse Sal cells by Western blottingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/26/2012
Entry Details Article
PubMed
TargetInsulin-like growth factor 1 receptor(Mouse)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 13nMAssay Description:Inhibition of IGF-1R in mouse IGF-1R-Sal cells assessed as inhibition of p44 MAPK phosphorylation at 0.1 to 1000 nmol/L incubated for 1 hr by Western...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetInsulin-like growth factor 1 receptor(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 21nMAssay Description:Inhibition of IGF-1R phosphorylation in human GEO cells at 0.1 to 1000 nmol/L incubated for 1 hr by Western blotting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetRAC-alpha serine/threonine-protein kinase(Mouse)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 22nMAssay Description:Inhibition of Akt phosphorylation in mouse Sal cells by Western blottingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/26/2012
Entry Details Article
PubMed
TargetInsulin-like growth factor 1 receptor(Mouse)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 22nMAssay Description:Inhibition of IGF-1R in mouse IGF-1R-Sal cells assessed as inhibition of Akt phosphorylation at Ser473 at 0.1 to 1000 nmol/L incubated for 1 hr by We...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetAurora kinase B(Human)TBA
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 25nMAssay Description:Inhibition of recombinant AurB (unknown origin) incubated for 60 mins in presence of ATP by electrophoretic caliper fluorescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 44nMAssay Description:Inhibition of recombinant RON (unknown origin) incubated for 60 mins in presence of ATP by electrophoretic caliper fluorescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataKd:  50nMAssay Description:Binding affinity to IRR (unknown origin) by phage based competition assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 144nMAssay Description:Inhibition of Met autophosphorylation in human GTL 16 cell line by Western blotting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 170nMAssay Description:Inhibition of recombinant Flt-3 (unknown origin) incubated for 60 mins in presence of ATP by electrophoretic caliper fluorescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataKd:  200nMAssay Description:Binding affinity to TRKC (unknown origin) by phage based competition assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataKd:  200nMAssay Description:Binding affinity to NEK6 (unknown origin) by phage based competition assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataKd:  300nMAssay Description:Binding affinity to PYK2 (unknown origin) by phage based competition assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 347nMAssay Description:Inhibition of recombinant Jak2 (unknown origin) incubated for 60 mins in presence of ATP by electrophoretic caliper fluorescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetAngiopoietin-1 receptor(Human)TBA
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataKd:  350nMAssay Description:Binding affinity to TIE2 (unknown origin) by phage based competition assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetHigh affinity nerve growth factor receptor(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataKd:  450nMAssay Description:Binding affinity to TRKA (unknown origin) by phage based competition assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetEphrin type-A receptor 2 [596-900](Human)
Technical University of Munich

LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataKd:  525nMAssay Description:Kinobeads competition assays were performed in 96-well format as previously described using mixed protein lysates of four cancer cell lines (K-562, M...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/23/2017
Entry Details Article
PubMed
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataKd:  600nMAssay Description:Binding affinity to TIE1 (unknown origin) by phage based competition assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataKd:  650nMAssay Description:Binding affinity to NEK7 (unknown origin) by phage based competition assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataKd:  750nMAssay Description:Binding affinity to PLK4 (unknown origin) by phage based competition assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 785nMAssay Description:Inhibition of recombinant GSK-3b (unknown origin) incubated for 60 mins in presence of ATP by electrophoretic caliper fluorescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 795nMAssay Description:Inhibition of recombinant CDK2/Cyclin E (unknown origin) incubated for 60 mins in presence of ATP by electrophoretic caliper fluorescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetInsulin-like growth factor 1 receptor(Human)
University of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataKd:  800nMAssay Description:Binding affinity to IGF1R (unknown origin) by phage based competition assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataKd:  850nMAssay Description:Binding affinity to DDR1 (unknown origin) by phage based competition assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 919nMAssay Description:Inhibition of recombinant MK2 (unknown origin) incubated for 60 mins in presence of ATP by electrophoretic caliper fluorescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 1.02E+3nMAssay Description:Inhibition of TrkA autophosphorylation in rat CD8-TrkA cells by Western blotting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 1.04E+3nMAssay Description:Inhibition of CDK2/Cyclin E after 60 mins by fluorescence electrophoresisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/26/2012
Entry Details Article
PubMed
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 1.22E+3nMAssay Description:Inhibition of recombinant Lck (unknown origin) incubated for 60 mins in presence of ATP by electrophoretic caliper fluorescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 1.53E+3nMAssay Description:Inhibition of recombinant SRC (unknown origin) incubated for 60 mins in presence of ATP by electrophoretic caliper fluorescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 1.61E+3nMAssay Description:Inhibition of recombinant PKA (unknown origin) incubated for 60 mins in presence of ATP by electrophoretic caliper fluorescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataKd:  1.70E+3nMAssay Description:Binding affinity to DCAMKL1 (unknown origin) by phage based competition assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataKd:  1.80E+3nMAssay Description:Binding affinity to NUAK2 (unknown origin) by phage based competition assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataKd:  2.00E+3nMAssay Description:Binding affinity to MET (unknown origin) by phage based competition assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 2.53E+3nMAssay Description:Inhibition of recombinant PKCalpha (unknown origin) incubated for 60 mins in presence of ATP by electrophoretic caliper fluorescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetSerine/threonine-protein kinase LMTK3(Human)
San Diego State University

Curated by ChEMBL
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataIC50: 3.16E+3nMAssay Description:Inhibition of LMTK3 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
LigandPNGBDBM50299148(1-{4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo...)
Affinity DataKd:  3.40E+3nMAssay Description:Binding affinity to AXL (unknown origin) by phage based competition assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
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