crenolanib [Ligand Id: 7882] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2105728 (CP 868596, ARO 002, CP-868,596, CP-868596, Crenolanib, ARO-002)
  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • platelet derived growth factor receptor alpha in Human [GtoPdb: 1803] [UniProtKB: P16234]
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  • platelet derived growth factor receptor beta in Human [GtoPdb: 1804] [UniProtKB: P09619]
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  • KIT proto-oncogene, receptor tyrosine kinase in Human [GtoPdb: 1805] [UniProtKB: P10721]
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  • colony stimulating factor 1 receptor in Human [GtoPdb: 1806] [UniProtKB: P07333]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Binding affinity to human FLT3 ITD/F691L double mutant expressed in baculovirus expression system B 7.66 pKd 22 nM Kd J Med Chem (2019) 62: 2428-2446 [PMID:30742435]
GtoPdb - - 9.13 pKd 0.74 nM Kd Clin Cancer Res (2012) 18: 4375-84 [PMID:22745105]
ChEMBL Binding affinity to human FLT3 ITD mutant expressed in baculovirus expression system B 9.59 pKd 0.26 nM Kd J Med Chem (2019) 62: 2428-2446 [PMID:30742435]
ChEMBL Binding affinity to human FLT3 D835H mutant expressed in baculovirus expression system B 9.8 pKd 0.16 nM Kd J Med Chem (2019) 62: 2428-2446 [PMID:30742435]
ChEMBL Binding affinity to non-auto-inhibited form of wild type human N-terminal GST-tagged FLT3 expressed in baculovirus expression B 9.82 pKd 0.15 nM Kd J Med Chem (2019) 62: 2428-2446 [PMID:30742435]
ChEMBL Inhibition of FLT3 ITD/D835H double mutant (unknown origin) B 7.46 pIC50 35 nM IC50 Eur J Med Chem (2019) 178: 468-483 [PMID:31207462]
ChEMBL Inhibition of FLT3 ITD/D835Y double mutant (unknown origin) B 7.46 pIC50 35 nM IC50 Eur J Med Chem (2019) 178: 468-483 [PMID:31207462]
ChEMBL Competitive inhibition of FLT3 D835Y mutant (unknown origin) in presence of ATP B 8.4 pIC50 4 nM IC50 ACS Med. Chem. Lett. (2016) 7: 476-481 [PMID:27190596]
ChEMBL Competitive inhibition of FLT3 ITD mutant (unknown origin) in presence of ATP B 8.52 pIC50 3 nM IC50 ACS Med. Chem. Lett. (2016) 7: 476-481 [PMID:27190596]
ChEMBL Inhibition of FLT3 D835H mutant (unknown origin) B 9.52 pIC50 0.3 nM IC50 Eur J Med Chem (2019) 178: 468-483 [PMID:31207462]
ChEMBL Inhibition of FLT3 D835Y mutant (unknown origin) B 10.22 pIC50 0.06 nM IC50 Eur J Med Chem (2019) 178: 468-483 [PMID:31207462]
platelet derived growth factor receptor alpha in Human [GtoPdb: 1803] [UniProtKB: P16234]
GtoPdb - - 8.68 pKd 2.1 nM Kd Clin Cancer Res (2012) 18: 4375-84 [PMID:22745105]
platelet derived growth factor receptor beta in Human [GtoPdb: 1804] [UniProtKB: P09619]
GtoPdb - - 8.49 pKd 3.2 nM Kd Clin Cancer Res (2012) 18: 4375-84 [PMID:22745105]
KIT proto-oncogene, receptor tyrosine kinase in Human [GtoPdb: 1805] [UniProtKB: P10721]
GtoPdb - - 7.11 pKd 78 nM Kd Clin Cancer Res (2012) 18: 4375-84 [PMID:22745105]
colony stimulating factor 1 receptor in Human [GtoPdb: 1806] [UniProtKB: P07333]
GtoPdb - - 7.52 pKd 30 nM Kd Clin Cancer Res (2012) 18: 4375-84 [PMID:22745105]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]