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 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 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 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]
ChEMBL	Inhibition of LRRK2 (1326 to 2527 residues) in HEK293 cell lysate measured after 15 mins in presence of ATP	B	7.89	pIC50	13	nM	IC50	Eur J Med Chem (2023) 256: 115475-115475 [PMID:37201428]
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 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]
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 LRRK2 (unknown origin)	B	8.22	pIC50	6	nM	IC50	J Med Chem (2015) 58: 6733-6746 [PMID:25915084]
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 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 LRRK2 G2019S mutant in HEK293 cell lysate measured after 15 mins in presence of ATP	B	8.22	pIC50	6	nM	IC50	Eur J Med Chem (2023) 256: 115475-115475 [PMID:37201428]
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 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]