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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 |
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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 | Binding affinity to human RSK1 assessed as dissociation constant | B | 5.45 | pKd | 3546 | nM | Kd | J Med Chem (2016) 59: 9305-9320 [PMID:27559828] |
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] |
ChEMBL | Inhibition of RSK1 (unknown origin) by mobility shift assay | B | 7.51 | pIC50 | 31 | nM | IC50 | J Med Chem (2016) 59: 9305-9320 [PMID:27559828] |
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 human RSK3 | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2016) 59: 9305-9320 [PMID:27559828] |
ChEMBL | Inhibition of RSK3 (unknown origin) | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2016) 59: 9305-9320 [PMID:27559828] |
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] |
ChEMBL | Inhibition of RSK2 (unknown origin) | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (2016) 59: 9305-9320 [PMID:27559828] |
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) | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2016) 59: 9305-9320 [PMID:27559828] |
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 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]