BI-D1870 [Ligand Id: 8038] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL573107 (BI-D1870) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885] | ||||||||
| ChEMBL | Binding affinity to BRD4 bromodomain 1 (unknown origin) by ITC assay | B | 5.46 | pKd | 3500 | nM | Kd | Bioorg Med Chem (2020) 28: 115303-115303 [PMID:31982240] |
| casein kinase 1 alpha 1/Casein kinase I alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729] | ||||||||
| ChEMBL | Inhibition of CK1 using KRRRALS(p)VASLPGL as substrate after 40 mins by scintillation counter | B | 6.35 | pIC50 | 450 | nM | IC50 | Eur J Med Chem (2012) 56: 30-38 [PMID:22944772] |
| ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418] | ||||||||
| ChEMBL | Inhibition of RSK1 (unknown origin) using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK a substrate by [32P] gammaATP assay | B | 7.51 | pIC50 | 31 | nM | IC50 | Bioorg Med Chem (2020) 28: 115303-115303 [PMID:31982240] |
| GtoPdb | - | - | 7.51 | pIC50 | 31 | nM | IC50 | Biochem J (2007) 401: 29-38 [PMID:17040210] |
| ChEMBL | Inhibition of RSK1 (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem (2020) 28: 115303-115303 [PMID:31982240] |
| ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5528] [GtoPdb: 1527] [UniProtKB: Q63531] | ||||||||
| ChEMBL | Inhibition of N-terminal HA-tagged rat RSK1 using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK-peptide as substrate in presence of [gamma-32P]ATP | B | 7.51 | pIC50 | 31 | nM | IC50 | J Med Chem (2021) 64: 13572-13587 [PMID:34496560] |
| ribosomal protein S6 kinase A2/Ribosomal protein S6 kinase alpha 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3906] [GtoPdb: 1529] [UniProtKB: Q15349] | ||||||||
| GtoPdb | - | - | 7.74 | pIC50 | 18 | nM | IC50 | Biochem J (2007) 401: 29-38 [PMID:17040210] |
| ChEMBL | Inhibition of RSK3 (unknown origin) using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK a substrate by [32P] gammaATP assay | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem (2020) 28: 115303-115303 [PMID:31982240] |
| ChEMBL | Inhibition of RSK3 (unknown origin) | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2021) 64: 13572-13587 [PMID:34496560] |
| ChEMBL | Inhibition of RSK3 (unknown origin) | B | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem (2020) 28: 115303-115303 [PMID:31982240] |
| ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812] | ||||||||
| ChEMBL | Inhibition of full length human GST-tagged RSK2 using Ulight-rpS6 as substrate incubated for 1 hr in presence of ATP by TR FRET assay | B | 4.63 | pIC50 | 23300 | nM | IC50 | Bioorg Med Chem (2020) 28: 115303-115303 [PMID:31982240] |
| ChEMBL | Inhibition of RSK2 (unknown origin) using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK a substrate by [32P] gammaATP assay | B | 7.62 | pIC50 | 24 | nM | IC50 | Bioorg Med Chem (2020) 28: 115303-115303 [PMID:31982240] |
| ChEMBL | Inhibition of His6-tagged human RSK2 using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK-peptide as substrate in presence of [gamma-32P]ATP | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (2021) 64: 13572-13587 [PMID:34496560] |
| GtoPdb | - | - | 7.62 | pIC50 | 24 | nM | IC50 | Biochem J (2007) 401: 29-38 [PMID:17040210] |
| ChEMBL | Inhibition of RSK2 (unknown origin) using Ulight-rpS6 as substrate incubated for 1 hr in presence of ATP by TR FRET assay | B | 7.65 | pIC50 | 22.6 | nM | IC50 | Bioorg Med Chem (2021) 41: 116220-116220 [PMID:34034149] |
| ChEMBL | Inhibition of RSK2 (unknown origin) | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem (2020) 28: 115303-115303 [PMID:31982240] |
| ChEMBL | Inhibition of RSK2 in human MOLM-13 assessed as reduction in cell viability measured after 72 hrs by MTS assay | B | 5.59 | pEC50 | 2600 | nM | EC50 | Bioorg Med Chem (2021) 41: 116220-116220 [PMID:34034149] |
| ribosomal protein S6 kinase A6/Ribosomal protein S6 kinase alpha 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4924] [GtoPdb: 1530] [UniProtKB: Q9UK32] | ||||||||
| GtoPdb | - | - | 7.82 | pIC50 | 15 | nM | IC50 | Biochem J (2007) 401: 29-38 [PMID:17040210] |
| ChEMBL | Inhibition of RSK4 (unknown origin) using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK a substrate by [32P] gammaATP assay | B | 7.82 | pIC50 | 15 | nM | IC50 | Bioorg Med Chem (2020) 28: 115303-115303 [PMID:31982240] |
| ChEMBL | Inhibition of RSK4 (unknown origin) | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2021) 64: 13572-13587 [PMID:34496560] |
| ChEMBL | Inhibition of RSK4 (unknown origin) incubated for 40 mins in presence of ATP and lipid substrate by Kinase-Glo plus luminescence assay | B | 7.94 | pIC50 | 11.5 | nM | IC50 | J Med Chem (2021) 64: 13572-13587 [PMID:34496560] |
| VRK serine/threonine kinase 1/Serine/threonine-protein kinase VRK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293199] [GtoPdb: 2275] [UniProtKB: Q99986] | ||||||||
| ChEMBL | Inhibition of full length wild-type VRK1 (unknown origin) expressed in insect cells using ULight-Histone 3-Thr3 peptide as substrate incubated for 30 mins followed by substrate addition further incubated for 75 mins by fluorescence based assay | B | 7.48 | pIC50 | 33 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1266-1271 [PMID:31531195] |
| Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
| ChEMBL | Binding affinity to wild type human C-terminal thrombin cleavage site-fused/ 6xHis-tagged JAK2 JH2 pseudokinase domain (536 to 812 residues) expressed in baculovirus infected sf9 insect cells measured for 1 hr in presence of fluorescein conjugate tracer by competitive fluorescence polarization assay | B | 5.7 | pKd | 2000 | nM | Kd | J Med Chem (2020) 63: 5324-5340 [PMID:32329617] |
| ChEMBL | Binding affinity to human C-terminal His8-tagged JAK2 pseudokinase (513 to 827 residues) expressed in baculovirus infected Hi-5 cells by intrinsic tryptophan fluorescence assay | B | 6.21 | pKd | 620 | nM | Kd | J Med Chem (2020) 63: 5324-5340 [PMID:32329617] |
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]
