RN486 [Ligand Id: 8249] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2057918 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG | B | 5.85 | pIC50 | 1400 | nM | IC50 | Bioorg Med Chem (2021) 40: 116163-116163 [PMID:33932711] |
| STE20 like kinase/Serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4202] [GtoPdb: 2200] [UniProtKB: Q9H2G2] | ||||||||
| GtoPdb | - | - | 7.37 | pKd | 43 | nM | Kd | J Pharmacol Exp Ther (2012) 341: 90-103 [PMID:22228807] |
| ChEMBL | Inhibition of SLK (unknown origin) | B | 7.37 | pIC50 | 43 | nM | IC50 | Eur J Med Chem (2018) 151: 315-326 [PMID:29631132] |
| BMX non-receptor tyrosine kinase/Tyrosine-protein kinase BMX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813] | ||||||||
| ChEMBL | Inhibition of human BMX | B | 7.21 | pIC50 | 62.04 | nM | IC50 | Bioorg Med Chem (2021) 40: 116163-116163 [PMID:33932711] |
| Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] | ||||||||
| GtoPdb | - | - | 9.51 | pKd | 0.31 | nM | Kd | J Pharmacol Exp Ther (2012) 341: 90-103 [PMID:22228807] |
| ChEMBL | Inhibition of BTK in human PBMC | B | 7.41 | pIC50 | 39 | nM | IC50 | Bioorg Med Chem (2021) 40: 116163-116163 [PMID:33932711] |
| ChEMBL | Inhibition of BTK in human Ramos cells after 20 mins by fluorescence assay | B | 7.56 | pIC50 | 27.3 | nM | IC50 | Bioorg Med Chem (2015) 23: 891-901 [PMID:25596757] |
| ChEMBL | Inhibition of BTK in human Ramos cells assessed as inhibition of anti human IgM-induced calcium influx preincubated for 20 mins in dark followed by anti human IgM induction for 8 mins by FLIPR assay | B | 7.56 | pIC50 | 27.3 | nM | IC50 | Bioorg Med Chem (2015) 23: 4344-4353 [PMID:26169764] |
| ChEMBL | Inhibition of BTK in human Ramos cells assessed as reduction in IgM-induced calcium influx incubated for 20 mins by Fluo-4 dye based fluorescence assay | B | 7.57 | pIC50 | 27 | nM | IC50 | Bioorg Med Chem (2015) 23: 348-364 [PMID:25515957] |
| ChEMBL | Inhibition of BTK in human whole blood | B | 7.59 | pIC50 | 26 | nM | IC50 | Bioorg Med Chem (2021) 40: 116163-116163 [PMID:33932711] |
| ChEMBL | Inhibition of recombinant human His-tagged full length BTK expressed in baculovirus using biotin labeled peptide substrate after 1 hr by HRTF kinase/TR-FRET assay | B | 7.88 | pIC50 | 13.2 | nM | IC50 | Bioorg Med Chem (2015) 23: 4344-4353 [PMID:26169764] |
| ChEMBL | Inhibition of BTK (unknown origin) after 1 hr by TR-FRET analysis | B | 7.88 | pIC50 | 13.2 | nM | IC50 | Bioorg Med Chem (2015) 23: 891-901 [PMID:25596757] |
| ChEMBL | Inhibition of BTK (unknown origin) using biotin-labeled peptide substrate incubated for 1 hr by TR-FRET based HTRF kinase assay | B | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem (2015) 23: 348-364 [PMID:25515957] |
| ChEMBL | Inhibition of BTK (unknown origin) assessed as reduction in TNF production | B | 8.15 | pIC50 | 7 | nM | IC50 | Eur J Med Chem (2018) 151: 315-326 [PMID:29631132] |
| ChEMBL | Inhibition of BTK (unknown origin) | B | 8.4 | pIC50 | 4 | nM | IC50 | Eur J Med Chem (2018) 151: 315-326 [PMID:29631132] |
| ChEMBL | Inhibition of human BTK | B | 8.65 | pIC50 | 2.25 | nM | IC50 | Bioorg Med Chem (2021) 40: 116163-116163 [PMID:33932711] |
| ChEMBL | Inhibition of BTK (unknown origin) | B | 9.05 | pIC50 | 0.9 | nM | IC50 | Bioorg Med Chem (2021) 40: 116163-116163 [PMID:33932711] |
| ChEMBL | Competitive inhibition of BTK by TR-FRET based competitive assay | B | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (2012) 55: 4539-4550 [PMID:22394077] |
| FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FGR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769] | ||||||||
| ChEMBL | Inhibition of human FGR | B | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem (2021) 40: 116163-116163 [PMID:33932711] |
| tec protein tyrosine kinase/Tyrosine-protein kinase TEC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4246] [GtoPdb: 2238] [UniProtKB: P42680] | ||||||||
| ChEMBL | Inhibition of TEC (unknown origin) | B | 7.19 | pIC50 | 64 | nM | IC50 | Eur J Med Chem (2018) 151: 315-326 [PMID:29631132] |
| ChEMBL | Inhibition of human TEC | B | 8.24 | pIC50 | 5.69 | nM | IC50 | Bioorg Med Chem (2021) 40: 116163-116163 [PMID:33932711] |
| YES proto-oncogene 1, Src family tyrosine kinase/Tyrosine-protein kinase YES in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073] [GtoPdb: 2284] [UniProtKB: P07947] | ||||||||
| ChEMBL | Inhibition of human YES1 | B | 5.8 | pIC50 | 1592 | nM | IC50 | Bioorg Med Chem (2021) 40: 116163-116163 [PMID:33932711] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
