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-QHCPKHFHSA-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 22 hits for monomerid = 50299148   

TargetEphrin type-A receptor 2 [596-900](Homo sapiens (Human))
Technical University Of Munich

LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
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 DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase LMTK3(Homo sapiens)
San Diego State University

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50:  3.16E+3nMAssay Description:Inhibition of LMTK3 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Bristol-Myers Squibb Research And Development

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50:  2.10nMAssay Description:Inhibition of IGF1R in IGF1R-SAL cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50: >4.00E+4nMAssay Description:Inhibition of CYP3A4 using 7-benzyloxy-4-trifluoromethylcoumarin as substrateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50:  7.00E+3nMAssay Description:Inhibition of CYP3A4 using 7-benzyloxy-resorufin as substrateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C19(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50:  1.10E+4nMAssay Description:Inhibition of CYP2C19More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C9(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50:  2.30E+4nMAssay Description:Inhibition of CYP2C9More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50: >4.00E+4nMAssay Description:Inhibition of CYP2D6More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 1A2(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50: >4.00E+4nMAssay Description:Inhibition of CYP1A2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetRAC-alpha serine/threonine-protein kinase(Mus musculus)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50:  22nMAssay Description:Inhibition of Akt phosphorylation in mouse Sal cells by western blottingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Mus musculus)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50:  13nMAssay Description:Inhibition of IGF1R phosphorylation in mouse Sal cells by western blottingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedMMDB

TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Bristol-Myers Squibb Research And Development

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50:  2nMAssay Description:Inhibition of IGF1R after 60 mins by fluorescence electrophoresisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 2/G1/S-specific cyclin-E1/G1/S-specific cyclin-E2(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50:  1.04E+3nMAssay Description:Inhibition of CDK2/Cyclin E after 60 mins by fluorescence electrophoresisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBroad substrate specificity ATP-binding cassette transporter ABCG2(Homo sapiens (Human))
Rheinische Friedrich-Wilhelms-University Of Bonn

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50:  1.02E+4nMAssay Description:Inhibition of ABCG2 (unknown origin) expressed in MDCK2 cells co-expressing BCRP (unknown origin) assessed as effect on pheophorbide A accumulation p...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-dependent translocase ABCB1(Homo sapiens (Human))
Rheinische Friedrich-Wilhelms-University Of Bonn

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50:  1.77E+4nMAssay Description:Inhibition of ABCB1 in human A2780/ADR cells preincubated for 30 mins followed by calcein AM addition and measured at 60 secs time interval by fluore...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMultidrug resistance-associated protein 1(Homo sapiens (Human))
Rheinische Friedrich-Wilhelms-University Of Bonn

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50:  3.63E+4nMAssay Description:Inhibition of ABCC1 in human H69AR cells preincubated for 30 mins followed by calcein-AM addition measured at 60 secs time interval by fluorescence a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin receptor(Homo sapiens (Human))
University Of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50:  1.70nMAssay Description:Inhibition of IR (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Bristol-Myers Squibb Research And Development

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of IGF-1R (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
University Of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50:  7nMAssay Description:Inhibition of TRKA (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBDNF/NT-3 growth factors receptor(Homo sapiens (Human))
University Of Arkansas For Medical Sciences

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50:  4nMAssay Description:Inhibition of TRKB (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Bristol-Myers Squibb Research And Development

Curated by ChEMBL
LigandPNGBDBM50299148((S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrro...)
Affinity DataIC50:  8.40nMAssay Description:Inhibition of IGF1RMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed