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 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]
