ChEMBL ligand: CHEMBL2012582
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!

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 recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by ITC analysis	B	6.71	pKd	194	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 MST assay	B	7.16	pKd	69	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	7.18	pKd	66	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	5.77	pKd	1700	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	6.15	pKd	700	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	6.41	pKd	390	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]
GtoPdb	Biochemical assay dissociation constant.	-	8.22	pKi	6	nM	Ki	Bioorg Med Chem Lett (2013) 23: 3690-6 [PMID:23721803]
ChEMBL	Inhibition of GST-tagged LRRK2 (1326 to 2527 amino acids) G2019S mutant (unknown origin)	B	8.22	pKi	6	nM	Ki	Bioorg Med Chem Lett (2013) 23: 3690-3696 [PMID:23721803]
ChEMBL	Inhibition of LRRK2 G2019S and A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate	B	5.51	pIC50	3080	nM	IC50	Bioorg Med Chem Lett (2012) 22: 1864-1869 [PMID:22335897]
ChEMBL	Inhibition of LRRK2 A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate	B	5.61	pIC50	2450	nM	IC50	Bioorg Med Chem Lett (2012) 22: 1864-1869 [PMID:22335897]
ChEMBL	Inhibition of recombinant catalytic human GST-tagged LLRK2 (970 to 2527 residues) expressed in baculovirus expression system using LRRKtide as substrate after 1 hr by alexaFluor-ADP-based FRET assay	B	7.7	pIC50	20	nM	IC50	Eur J Med Chem (2017) 138: 328-342 [PMID:28688273]
ChEMBL	Inhibition of recombinant catalytic human GST-tagged LLRK2 G2019S mutant (970 to 2527 residues) expressed in baculovirus expression system using LRRKtide as substrate after 1 hr by alexaFluor-ADP-based FRET assay	B	7.7	pIC50	20	nM	IC50	Eur J Med Chem (2017) 138: 328-342 [PMID:28688273]
ChEMBL	Inhibition of wild-type GST-tagged LRRK2 (1326 to 2527 aa)(unknown origin) stably expressed in HEK293 cell lysate using [gamma-32P] after 15 mins by Cerenkov counting method	B	7.89	pIC50	13	nM	IC50	Eur J Med Chem (2015) 95: 29-34 [PMID:25791676]
ChEMBL	Inhibition of wild type GST-tagged LRRK2 ((1326 to 2517 amino acids) (unknown origin)	B	7.89	pIC50	13	nM	IC50	Bioorg Med Chem Lett (2013) 23: 3690-3696 [PMID:23721803]
ChEMBL	Inhibition of wild-type LRRK2 expressed in HEK293 cells using nictide and [gamma32]ATP as substrate	B	7.89	pIC50	13	nM	IC50	Bioorg Med Chem Lett (2012) 22: 1864-1869 [PMID:22335897]
GtoPdb	With 0.1 mM ATP in the assay.	-	7.89	pIC50	13	nM	IC50	Nat Chem Biol (2011) 7: 203-5 [PMID:21378983]
ChEMBL	Inhibition of LRRK2 G2019S mutant (1326 to 252 aa) (unknown origin) stably expressed in HEK293 cell lysate using [gamma-32P] after 15 mins by Cerenkov counting method	B	8.1	pIC50	7.9	nM	IC50	Eur J Med Chem (2015) 95: 29-34 [PMID:25791676]
ChEMBL	Inhibition of GST-LRRK2 (1326 to 2527 residues) G2019S mutant (unknown origin) expressed in HEK293 cells incubated for 15 mins by cerenkov counting method	B	8.22	pIC50	6	nM	IC50	J Med Chem (2020) 63: 11330-11361 [PMID:32352776]
ChEMBL	Inhibition of LRRK2 G2019S mutant expressed in HEK293 cells using nictide and ATP as substrate	B	8.22	pIC50	6	nM	IC50	Bioorg Med Chem Lett (2012) 22: 1864-1869 [PMID:22335897]
ChEMBL	Inhibition of GST-tagged LRRK2 (1326 to 2527 amino acids) G2019S mutant (unknown origin)	B	8.22	pIC50	6	nM	IC50	Bioorg Med Chem Lett (2013) 23: 3690-3696 [PMID:23721803]
ChEMBL	Inhibition of LRRK2 (unknown origin)	B	8.22	pIC50	6	nM	IC50	J Med Chem (2015) 58: 6733-6746 [PMID:25915084]
ChEMBL	Inhibition of recombinant LRRK2 (unknown origin) using gamma-32P-ATP assessed as LRRKtide substrate phosphorylation level by autoradiography	B	8.46	pIC50	3.5	nM	IC50	Bioorg Med Chem Lett (2014) 24: 4630-4637 [PMID:25219901]

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]