ChEMBL ligand: CHEMBL1673046
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!
bromodomain testis associated/Bromodomain testis-specific protein in Human [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21] There should be some charts here, you may need to enable JavaScript!
protein tyrosine kinase 2/Focal adhesion kinase 1 in Human [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397] There should be some charts here, you may need to enable JavaScript!
leucine rich repeat kinase 2/Leucine-rich repeat serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL1075104] [GtoPdb: 2059] [UniProtKB: Q5S007] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase 7/Mitogen-activated protein kinase 7 in Human [ChEMBL: CHEMBL5332] [GtoPdb: 2093] [UniProtKB: Q13164] There should be some charts here, you may need to enable JavaScript!
tyrosine kinase non receptor 1/Non-receptor tyrosine-protein kinase TNK1 in Human [ChEMBL: CHEMBL5334] [GtoPdb: 2245] [UniProtKB: Q13470] There should be some charts here, you may need to enable JavaScript!
phosphatidylinositol 4-kinase alpha/PI4-kinase alpha subunit in Human [ChEMBL: CHEMBL3667] [GtoPdb: 2148] [UniProtKB: P42356] 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!
doublecortin like kinase 1/Serine/threonine-protein kinase DCLK1 in Human [ChEMBL: CHEMBL5683] [GtoPdb: 2005] [UniProtKB: O15075] There should be some charts here, you may need to enable JavaScript!
doublecortin like kinase 2/Serine/threonine-protein kinase DCLK2 in Human [ChEMBL: CHEMBL5519] [GtoPdb: 2006] [UniProtKB: Q8N568] There should be some charts here, you may need to enable JavaScript!
polo like kinase 4/Serine/threonine-protein kinase PLK4 in Human [ChEMBL: CHEMBL3788] [GtoPdb: 2171] [UniProtKB: O00444] There should be some charts here, you may need to enable JavaScript!
tyrosine kinase non receptor 2/Tyrosine kinase non-receptor protein 2 in Human [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912] 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	Inhibition of BRD4 (unknown origin)	B	5.8	pKd	1600	nM	Kd	Eur J Med Chem (2019) 178: 530-543 [PMID:31212132]
ChEMBL	Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by MST assay	B	6.1	pKd	800	nM	Kd	J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
ChEMBL	Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by ITC analysis	B	6.13	pKd	735	nM	Kd	J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
ChEMBL	Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by qPCR assay	B	6.69	pKd	205	nM	Kd	J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
bromodomain testis associated/Bromodomain testis-specific protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21]
ChEMBL	Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by ITC analysis	B	5.38	pKd	4200	nM	Kd	J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
ChEMBL	Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by MST assay	B	5.46	pKd	3500	nM	Kd	J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
ChEMBL	Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by qPCR assay	B	6.17	pKd	675	nM	Kd	J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
ChEMBL	Selectivity interaction (Kinase panel (KiNativ method in HeLa cells)) EUB0000122b PTK2	B	4.41	pIC50	39000	nM	IC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
leucine rich repeat kinase 2/Leucine-rich repeat serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075104] [GtoPdb: 2059] [UniProtKB: Q5S007]
ChEMBL	Inhibition of recombinant human GST-tagged LRRK2 catalytic domain (970 to 2527 residues) expressed in baculovirus expression system using LRRKtide as substrate measured after 1 hr by Alexa fluor-647 ADP tracer-based ADAPTA assay	B	7.34	pIC50	46	nM	IC50	J Med Chem (2020) 63: 7817-7826 [PMID:32530623]
mitogen-activated protein kinase 7/Mitogen-activated protein kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5332] [GtoPdb: 2093] [UniProtKB: Q13164]
ChEMBL	In vitro Erk5 : In vitro Erk5 binding assay: Ambit Kd values in nanomolar. Kd values generated by Ambit binding assay over a concentration range of the compound.	B	7.1	pKd	80	nM	Kd	US-9266890-B2. Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders (2016)
ChEMBL	Affinity Biochemical interaction (ATP-binding displacement assay) EUB0000122b MAPK7	B	7.1	pKd	80	nM	Kd	Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Selectivity interaction (Kinase panel (ATP-site competition binding assay)) EUB0000122b MAPK7	B	7.1	pKd	80	nM	Kd	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
GtoPdb	-	-	7.1	pKd	80	nM	Kd	Cancer Cell (2010) 18: 258-67 [PMID:20832753]
ChEMBL	Affinity On-target Cellular interaction (KiNativ assay (HeLa cell lysate)) EUB0000122b MAPK7	B	5.82	pIC50	1500	nM	IC50	Affinity On-target Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Inhibition of ERK5 in human HeLa cells incubated for 15 mins prior to ATP addition by KiNativ profiling method	B	6.52	pIC50	300	nM	IC50	Eur J Med Chem (2019) 178: 530-543 [PMID:31212132]
ChEMBL	Inhibition of EGF-induced BMK1 autophosphorylation in human HeLa cells by SDS-PAGE analysis	B	6.62	pIC50	240	nM	IC50	ACS Med Chem Lett (2011) 2: 195-200 [PMID:21412406]
ChEMBL	Inhibition of His-tagged MAP2K5 activated N-terminal GST-tagged recombinant human ERK5 (1 to 398 residues) expressed in Escherichia coli using biotin-Ahx-PPGDYSTTPGGTLFSTTPGGTRI peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins in presence of ATP by TR-FRET assay	B	6.7	pIC50	200	nM	IC50	J Med Chem (2019) 62: 928-940 [PMID:30563338]
ChEMBL	Affinity Phenotypic Cellular interaction (Reduction of BMK1-dependent transactivating activity of MEF2C) EUB0000122b MAPK7	B	5.3	pEC50	<5000	nM	EC50	Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
tyrosine kinase non receptor 1/Non-receptor tyrosine-protein kinase TNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5334] [GtoPdb: 2245] [UniProtKB: Q13470]
GtoPdb	-	-	6.05	pKd	890	nM	Kd	Cancer Cell (2010) 18: 258-67 [PMID:20832753]
ChEMBL	Selectivity interaction (Kinase panel (ATP-site competition binding assay)) EUB0000122b TNK1	B	6.05	pKd	890	nM	Kd	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Selectivity interaction (Kinase panel (KiNativ method in HeLa cells)) EUB0000122b TNK1	B	5	pIC50	10000	nM	IC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
phosphatidylinositol 4-kinase alpha/PI4-kinase alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3667] [GtoPdb: 2148] [UniProtKB: P42356]
ChEMBL	Selectivity interaction (Kinase panel (KiNativ method in HeLa cells)) EUB0000122b PI4KA	B	4.44	pIC50	36000	nM	IC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ribosomal protein S6 kinase A2/Ribosomal protein S6 kinase alpha 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3906] [GtoPdb: 1529] [UniProtKB: Q15349]
ChEMBL	Selectivity interaction (Kinase panel (KiNativ method in HeLa cells)) EUB0000122b RPS6KA1	B	4.54	pIC50	29000	nM	IC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812]
ChEMBL	Selectivity interaction (Kinase panel (KiNativ method in HeLa cells)) EUB0000122b RPS6KA3	B	4.33	pIC50	47000	nM	IC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
doublecortin like kinase 1/Serine/threonine-protein kinase DCLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5683] [GtoPdb: 2005] [UniProtKB: O15075]
ChEMBL	Inhibition of recombinant human N-terminal His6-tagged DCLK1 (G351 to H689 residues) expressed in Escherichia coli BL21 DE3 using 5-FAM-KKLRRTLSVA-COOH as substrate measured after 2 hrs by mobility shift assay	B	6.15	pIC50	716	nM	IC50	J Med Chem (2020) 63: 7817-7826 [PMID:32530623]
doublecortin like kinase 2/Serine/threonine-protein kinase DCLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5519] [GtoPdb: 2006] [UniProtKB: Q8N568]
GtoPdb	-	-	6.72	pKd	190	nM	Kd	Cancer Cell (2010) 18: 258-67 [PMID:20832753]
ChEMBL	Selectivity interaction (Kinase panel (ATP-site competition binding assay)) EUB0000122b DCLK2	B	6.72	pKd	190	nM	Kd	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
polo like kinase 4/Serine/threonine-protein kinase PLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3788] [GtoPdb: 2171] [UniProtKB: O00444]
GtoPdb	-	-	6.22	pKd	600	nM	Kd	Cancer Cell (2010) 18: 258-67 [PMID:20832753]
ChEMBL	Selectivity interaction (Kinase panel (ATP-site competition binding assay)) EUB0000122b PLK4	B	6.22	pKd	600	nM	Kd	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
tyrosine kinase non receptor 2/Tyrosine kinase non-receptor protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912]
ChEMBL	Selectivity interaction (Kinase panel (KiNativ method in HeLa cells)) EUB0000122b TNK2	B	4.74	pIC50	18000	nM	IC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3

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]