AC710 [Ligand Id: 8095] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2206278 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| colony stimulating factor 1 receptor in Human [GtoPdb: 1806] [UniProtKB: P07333] | ||||||||
| GtoPdb | - | - | 8.8 | pKd | 1.57 | nM | Kd | ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421] |
| colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5570] [GtoPdb: 1806] [UniProtKB: P09581] | ||||||||
| ChEMBL | Inhibition of CSF1R in mouse M-NFS-60 cells assessed as inhibition of cell proliferation after 72 hrs by Celltiter-Blue assay | B | 7.33 | pIC50 | 46.3 | nM | IC50 | ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421] |
| colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333] | ||||||||
| GtoPdb | - | - | 8.8 | pKd | 1.57 | nM | Kd | ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421] |
| ChEMBL | Binding affinity to CSF1R expressed in HEK-293 cells after 1 hr | B | 8.8 | pKd | 1.57 | nM | Kd | ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421] |
| ChEMBL | Inhibition of M-CSF-induced FK506 -fussed CSF1R phosphorylation expressed in HEK293 cells after 2 hrs by sandwich ELISA | B | 7.98 | pIC50 | 10.5 | nM | IC50 | ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421] |
| platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234] | ||||||||
| ChEMBL | Binding affinity to PDGFRalpha expressed in HEK-293 cells | B | 8.89 | pKd | 1.3 | nM | Kd | ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421] |
| GtoPdb | - | - | 8.89 | pKd | 1.3 | nM | Kd | ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421] |
| ChEMBL | Inhibition of PDGFRbeta phosphorylation in human MG63 cells | B | 8.11 | pIC50 | 7.7 | nM | IC50 | ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421] |
| platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619] | ||||||||
| GtoPdb | - | - | 9 | pKd | 1 | nM | Kd | ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421] |
| ChEMBL | Binding affinity to PDGFRbeta expressed in HEK-293 cells | B | 9 | pKd | 1 | nM | Kd | ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421] |
| KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] | ||||||||
| GtoPdb | - | - | 9 | pKd | 1 | nM | Kd | ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421] |
| ChEMBL | Binding affinity to KIT expressed in HEK-293 cells | B | 9 | pKd | 1 | nM | Kd | ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421] |
| ChEMBL | Inhibition of KIT phosphorylation in human H526 cells | B | 8.92 | pIC50 | 1.2 | nM | IC50 | ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421] |
| fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| GtoPdb | - | - | 9.3 | pKd | 0.5 | nM | Kd | ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421] |
| ChEMBL | Binding affinity to FLT3 expressed in HEK-293 cells after 1 hr | B | 9.3 | pKd | 0.5 | nM | Kd | ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421] |
| ChEMBL | Inhibition of FLT3 phosphorylation in human MV4-11 cells | B | 8.7 | pIC50 | 2 | nM | IC50 | ACS Med Chem Lett (2012) 3: 997-1002 [PMID:24900421] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
