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!
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!
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 in Human [GtoPdb: 2006] [UniProtKB: Q8N568] There should be some charts here, you may need to enable JavaScript!
polo like kinase 4 in Human [GtoPdb: 2171] [UniProtKB: O00444] There should be some charts here, you may need to enable JavaScript!
tyrosine kinase non receptor 1 in Human [GtoPdb: 2245] [UniProtKB: Q13470] 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]
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)
GtoPdb	-	-	7.1	pKd	80	nM	Kd	Cancer Cell (2010) 18: 258-67 [PMID:20832753]
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]
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 in Human [GtoPdb: 2006] [UniProtKB: Q8N568]
GtoPdb	-	-	6.72	pKd	190	nM	Kd	Cancer Cell (2010) 18: 258-67 [PMID:20832753]
polo like kinase 4 in Human [GtoPdb: 2171] [UniProtKB: O00444]
GtoPdb	-	-	6.22	pKd	600	nM	Kd	Cancer Cell (2010) 18: 258-67 [PMID:20832753]
tyrosine kinase non receptor 1 in Human [GtoPdb: 2245] [UniProtKB: Q13470]
GtoPdb	-	-	6.05	pKd	890	nM	Kd	Cancer Cell (2010) 18: 258-67 [PMID:20832753]

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]