ChEMBL ligand: CHEMBL573107 (BI-D1870)
bromodomain containing 4/Bromodomain-containing protein 4 in Human [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885] There should be some charts here, you may need to enable JavaScript!
casein kinase 1 alpha 1/Casein kinase I alpha in Human [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729] There should be some charts here, you may need to enable JavaScript!
ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha 1 in Human [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418] ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha 1 in Rat [ChEMBL: CHEMBL5528] [GtoPdb: 1527] [UniProtKB: Q63531] There should be some charts here, you may need to enable JavaScript!
ribosomal protein S6 kinase A2/Ribosomal protein S6 kinase alpha 2 in Human [ChEMBL: CHEMBL3906] [GtoPdb: 1529] [UniProtKB: Q15349] There should be some charts here, you may need to enable JavaScript!
ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812] There should be some charts here, you may need to enable JavaScript!
ribosomal protein S6 kinase A6/Ribosomal protein S6 kinase alpha 6 in Human [ChEMBL: CHEMBL4924] [GtoPdb: 1530] [UniProtKB: Q9UK32] There should be some charts here, you may need to enable JavaScript!
VRK serine/threonine kinase 1/Serine/threonine-protein kinase VRK1 in Human [ChEMBL: CHEMBL1293199] [GtoPdb: 2275] [UniProtKB: Q99986] There should be some charts here, you may need to enable JavaScript!
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] There should be some charts here, you may need to enable JavaScript!

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	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]