XP-102 [Ligand Id: 13942] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4212692 (BI 882370, BI-882370, Xp 102, Xp-102) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056] | ||||||||
| GtoPdb | Binding to WT BRAF | - | 8.22 | pKd | 6 | nM | Kd | Mol Cancer Ther (2016) 15: 354-65 [PMID:26916115] |
| GtoPdb | Binding affinity for WT BRAF determined by KINOMEscan assay | - | 9.43 | pKd | 0.37 | nM | Kd | J Med Chem (2020) 63: 4069-4080 [PMID:32223235] |
| ChEMBL | Binding affinity to DNA-tagged BRAF (unknown origin) by KINOMEscan assay | B | 9.43 | pKd | 0.37 | nM | Kd | J Med Chem (2020) 63: 4069-4080 [PMID:32223235] |
| GtoPdb | Binding affinity for BRAF V600E determined by KINOMEscan assay | - | 9.48 | pKd | 0.33 | nM | Kd | J Med Chem (2020) 63: 4069-4080 [PMID:32223235] |
| ChEMBL | Binding affinity to DNA-tagged BRAF (unknown origin) V600E mutant by KINOMEscan assay | B | 9.48 | pKd | 0.33 | nM | Kd | J Med Chem (2020) 63: 4069-4080 [PMID:32223235] |
| ChEMBL | Inhibition of wild type BRAF (unknown origin) by Z'-LYTE assay | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (2018) 61: 5775-5793 [PMID:29461827] |
| ChEMBL | Inhibition of BRAF V600E mutant in human A375 cells assessed as reduction in ERK phosphorylation after 2 hrs by ELISA | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2018) 61: 5775-5793 [PMID:29461827] |
| ChEMBL | Inhibition of BRAF V600E mutant (unknown origin) by Z'-LYTE assay | B | 9.4 | pIC50 | 0.4 | nM | IC50 | J Med Chem (2018) 61: 5775-5793 [PMID:29461827] |
| ChEMBL | Inhibition of BRAF (unknown origin) | B | 9.4 | pIC50 | 0.4 | nM | IC50 | Bioorg Med Chem (2020) 28: 115493-115493 [PMID:32340792] |
| Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049] | ||||||||
| GtoPdb | Binding affinity for WT RAF1 (CRAF) | - | 8.52 | pKd | 3 | nM | Kd | Mol Cancer Ther (2016) 15: 354-65 [PMID:26916115] |
| ChEMBL | Inhibition of CRAF (unknown origin) by Z'-LYTE assay | B | 9.22 | pIC50 | 0.6 | nM | IC50 | J Med Chem (2018) 61: 5775-5793 [PMID:29461827] |
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]
