BMS-214662 [Ligand Id: 8026] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL351706 (Bms 214662, Bms-214662, BMS-214662) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| farnesyltransferase, CAAX box, subunit alpha/Geranylgeranyl transferase type I in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095164] [GtoPdb: 2825] [UniProtKB: P49354, P53609] | ||||||||
| ChEMBL | Inhibition of geranylgeranyl transferase (GGT1) using K-Ras as substrate | B | 5.64 | pIC50 | 2300 | nM | IC50 | J Med Chem (2000) 43: 3587-3595 [PMID:11020273] |
| ChEMBL | Inhibition of geranylgeranyl transferase (GGT1) using Ras-CVLL as substrate | B | 5.89 | pIC50 | 1300 | nM | IC50 | J Med Chem (2000) 43: 3587-3595 [PMID:11020273] |
| KRAS/GTPase KRas in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189121] [GtoPdb: 2824] [UniProtKB: P01116] | ||||||||
| ChEMBL | Inhibition of K-Ras (unknown origin) geranylgeranylation | B | 5.64 | pIC50 | 2300 | nM | IC50 | Eur J Med Chem (2021) 211: 113006-113006 [PMID:33228976] |
| ChEMBL | Inhibition of K-Ras (unknown origin) farnesylation | B | 8.08 | pIC50 | 8.4 | nM | IC50 | Eur J Med Chem (2021) 211: 113006-113006 [PMID:33228976] |
| ChEMBL | Inhibition of human K-ras | B | 8.08 | pIC50 | 8.4 | nM | IC50 | Eur J Med Chem (2021) 226: 113877-113877 [PMID:34624823] |
| farnesyltransferase, CAAX box, subunit alpha/farnesyltransferase, CAAX box, subunit beta/Protein farnesyltransferase in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094108] [GtoPdb: 2825, 2826] [UniProtKB: P49354, P49356] | ||||||||
| ChEMBL | Inhibition of farnesyltransferase (unknown origin) assessed as KRAS farnesylation | B | 8.08 | pIC50 | 8.4 | nM | IC50 | J Med Chem (2013) 56: 5219-5230 [PMID:23566315] |
| ChEMBL | Inhibitory concentration against farnesyltransferase was determined | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2004) 47: 1869-1878 [PMID:15055985] |
| ChEMBL | Inhibition of human FTase | B | 8.85 | pIC50 | 1.4 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6896-6902 [PMID:23036952] |
| ChEMBL | Inhibition of human recombinant FTase | B | 8.87 | pIC50 | 1.35 | nM | IC50 | J Med Chem (2018) 61: 3239-3252 [PMID:28505447] |
| ChEMBL | Inhibition of purified recombinant human farnesyltransferase (FT) | B | 8.87 | pIC50 | 1.35 | nM | IC50 | J Med Chem (2000) 43: 3587-3595 [PMID:11020273] |
| GtoPdb | - | - | 8.87 | pIC50 | 1.35 | nM | IC50 | J Med Chem (2000) 43: 3587-95 [PMID:11020273] |
| ChEMBL | Inhibition of farnesyltransferase | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 767-771 [PMID:14741286] |
| ChEMBL | Inhibition of farnesyltransferase (unknown origin) assessed as HRAS farnesylation | B | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (2013) 56: 5219-5230 [PMID:23566315] |
| ChEMBL | Inhibition of Farnesyltransferase | B | 9.15 | pIC50 | 0.7 | nM | IC50 | J Med Chem (2004) 47: 612-626 [PMID:14736242] |
| HRAS/Transforming protein p21/H-Ras-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2167] [GtoPdb: 2822] [UniProtKB: P01112] | ||||||||
| ChEMBL | Inhibition of HRAS (unknown origin) farnesylation | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Eur J Med Chem (2021) 211: 113006-113006 [PMID:33228976] |
| ChEMBL | Inhibition of human H-ras | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Eur J Med Chem (2021) 226: 113877-113877 [PMID:34624823] |
ChEMBL data shown on this page come from version 35:
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]
