belvarafenib [Ligand Id: 11544] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3977543 (Belvarafenib) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| discoidin domain receptor tyrosine kinase 2/Discoidin domain-containing receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5122] [GtoPdb: 1844] [UniProtKB: Q16832] | ||||||||
| ChEMBL | Kinase Activity: The compounds prepared in Examples were tested for inhibitory activity against FMS, DDR1 and DDR2 kinases using Kinase Screening and Profiling Service (Invitrogen, U.S.). | B | 7.36 | pIC50 | 44 | nM | IC50 | US-9156852-B2. Thieno[3,2-D]pyrimidine derivatives having inhibitory activity for protein kinases (2015) |
| discoidin domain receptor tyrosine kinase 1/Epithelial discoidin domain-containing receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5319] [GtoPdb: 1843] [UniProtKB: Q08345] | ||||||||
| ChEMBL | Kinase Activity: The compounds prepared in Examples were tested for inhibitory activity against FMS, DDR1 and DDR2 kinases using Kinase Screening and Profiling Service (Invitrogen, U.S.). | B | 7.64 | pIC50 | 23 | nM | IC50 | US-9156852-B2. Thieno[3,2-D]pyrimidine derivatives having inhibitory activity for protein kinases (2015) |
| colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333] | ||||||||
| ChEMBL | Kinase Activity: The compounds prepared in Examples were tested for inhibitory activity against FMS, DDR1 and DDR2 kinases using Kinase Screening and Profiling Service (Invitrogen, U.S.). | B | 8 | pIC50 | 10 | nM | IC50 | US-9156852-B2. Thieno[3,2-D]pyrimidine derivatives having inhibitory activity for protein kinases (2015) |
| ChEMBL | Kinase Activity: The compounds prepared in Examples were tested for inhibitory activity against FMS, DDR1 and DDR2 kinases using Kinase Screening and Profiling Service (Invitrogen, U.S.). | B | 8 | pIC50 | 10 | nM | IC50 | US-9156852-B2. Thieno[3,2-D]pyrimidine derivatives having inhibitory activity for protein kinases (2015) |
| Raf-1 proto-oncogene, serine/threonine kinase/RAF proto-oncogene serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049] | ||||||||
| ChEMBL | Inhibition of C-RAF (unknown origin) | B | 7.64 | pIC50 | 23 | nM | IC50 | Eur J Med Chem (2024) 275: 116631-116631 [PMID:38954961] |
| GtoPdb | - | - | 8.3 | pIC50 | 5 | nM | IC50 | WO2013100632A1. THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASES (2013) |
| ChEMBL | Kinase Activity: The compounds prepared in Examples were tested for inhibitory activity against three subtypes of RAF, i.e., RAF1 Y340D Y341D (C-RAF), B-RAF normal type and B-RAF.sup.V600E using Kinase Profiling Service (Invitrogen, U.S.) according to the manufacturer's instructions. The levels of enzymatic inhibition of the compounds were calculated as percent inhibition at various concentrations. | B | 8.3 | pIC50 | 5 | nM | IC50 | US-9156852-B2. Thieno[3,2-D]pyrimidine derivatives having inhibitory activity for protein kinases (2015) |
| A-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase A-Raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1169596] [GtoPdb: 1933] [UniProtKB: P10398] | ||||||||
| ChEMBL | Inhibition of ARAF (unknown origin) | B | 6.82 | pIC50 | 152 | nM | IC50 | Eur J Med Chem (2024) 275: 116631-116631 [PMID:38954961] |
| 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] | ||||||||
| ChEMBL | Inhibition of B-RAF (unknown origin) | B | 6.94 | pIC50 | 116 | nM | IC50 | Eur J Med Chem (2024) 275: 116631-116631 [PMID:38954961] |
| GtoPdb | In vitro Inhibition of wild type BRAF | - | 7.25 | pIC50 | 56 | nM | IC50 | WO2013100632A1. THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASES (2013) |
| ChEMBL | Kinase Activity: The compounds prepared in Examples were tested for inhibitory activity against three subtypes of RAF, i.e., RAF1 Y340D Y341D (C-RAF), B-RAF normal type and B-RAF.sup.V600E using Kinase Profiling Service (Invitrogen, U.S.) according to the manufacturer's instructions. The levels of enzymatic inhibition of the compounds were calculated as percent inhibition at various concentrations. | B | 7.25 | pIC50 | 56 | nM | IC50 | US-9156852-B2. Thieno[3,2-D]pyrimidine derivatives having inhibitory activity for protein kinases (2015) |
| ChEMBL | Inhibition of B-RAF V600E mutant (unknown origin) | B | 8.05 | pIC50 | 9 | nM | IC50 | Eur J Med Chem (2024) 275: 116631-116631 [PMID:38954961] |
| GtoPdb | In vitro Inhibition of BRAFV600E | - | 8.15 | pIC50 | 7 | nM | IC50 | WO2013100632A1. THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASES (2013) |
| ChEMBL | Kinase Activity: The compounds prepared in Examples were tested for inhibitory activity against three subtypes of RAF, i.e., RAF1 Y340D Y341D (C-RAF), B-RAF normal type and B-RAF.sup.V600E using Kinase Profiling Service (Invitrogen, U.S.) according to the manufacturer's instructions. The levels of enzymatic inhibition of the compounds were calculated as percent inhibition at various concentrations. | B | 8.15 | pIC50 | 7 | nM | IC50 | US-9156852-B2. Thieno[3,2-D]pyrimidine derivatives having inhibitory activity for protein kinases (2015) |
ChEMBL data shown on this page come from version 36:
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]
