ChEMBL ligand: CHEMBL4785363 (Ccs 1477, Ccs1477, CCS-1477, CCS1477, Inobrodib)
bromodomain containing 2/Bromodomain-containing protein 2 in Human [ChEMBL: CHEMBL1293289] [GtoPdb: 1944] [UniProtKB: P25440] There should be some charts here, you may need to enable JavaScript!
bromodomain containing 3/Bromodomain-containing protein 3 in Human [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059] There should be some charts here, you may need to enable JavaScript!
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 containing 9/Bromodomain-containing protein 9 in Human [ChEMBL: CHEMBL3108640] [GtoPdb: 2728] [UniProtKB: Q9H8M2] 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!
CREB binding lysine acetyltransferase/CREB-binding protein in Human [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793] There should be some charts here, you may need to enable JavaScript!
EP300 lysine acetyltransferase/Histone acetyltransferase p300 in Human [ChEMBL: CHEMBL3784] [GtoPdb: 2735] [UniProtKB: Q09472] There should be some charts here, you may need to enable JavaScript!
cereblon/Protein cereblon in Human [ChEMBL: CHEMBL3763008] [GtoPdb: 3086] [UniProtKB: Q96SW2] 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 2/Bromodomain-containing protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293289] [GtoPdb: 1944] [UniProtKB: P25440]
ChEMBL	Binding affinity to His6-tagged human BRD2 bromodomain-1 (77 to 194 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by ITC analysis	B	6.41	pKd	390	nM	Kd	J Med Chem (2022) 65: 785-810 [PMID:34962793]
ChEMBL	Inhibition of BRD2 BD2 (unknown origin) by Alphascreen assay	B	5.08	pIC50	8300	nM	IC50	J Med Chem (2024) 67: 18606-18628 [PMID:39356741]
ChEMBL	Inhibition of BRD2 BD1 (unknown origin) by Alphascreen assay	B	5.7	pIC50	2010	nM	IC50	J Med Chem (2024) 67: 18606-18628 [PMID:39356741]
bromodomain containing 3/Bromodomain-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059]
ChEMBL	Binding affinity to His6-tagged human BRD3 bromodomain-2 (306 to 416 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by ITC analysis	B	5.82	pKd	1510	nM	Kd	J Med Chem (2022) 65: 785-810 [PMID:34962793]
ChEMBL	Binding affinity to His6-tagged human BRD3 bromodomain-1 (24 to 144 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by ITC analysis	B	6.25	pKd	560	nM	Kd	J Med Chem (2022) 65: 785-810 [PMID:34962793]
ChEMBL	Inhibition of BRD3 BD2 (unknown origin) by Alphascreen assay	B	5.23	pIC50	5940	nM	IC50	J Med Chem (2024) 67: 18606-18628 [PMID:39356741]
ChEMBL	Inhibition of BRD3 BD1 (unknown origin) by Alphascreen assay	B	5.74	pIC50	1810	nM	IC50	J Med Chem (2024) 67: 18606-18628 [PMID:39356741]
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
ChEMBL	Binding affinity to His6-tagged human BRD4 bromodomain-1 (44 to 168 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by ITC analysis	B	6.44	pKd	360	nM	Kd	J Med Chem (2022) 65: 785-810 [PMID:34962793]
ChEMBL	Binding affinity to BRD4 (unknown origin) by SPR assay	B	6.65	pKd	222	nM	Kd	J Med Chem (2024) 67: 5351-5372 [PMID:38530938]
ChEMBL	Binding affinity to BRD4 (unknown origin) assessed as dissociation constant by SPR analysis	B	6.65	pKd	222	nM	Kd	J Med Chem (2024) 67: 5275-5304 [PMID:38477974]
ChEMBL	Inhibition of BRD4 BD2 (unknown origin) by Alphascreen assay	B	5	pIC50	>10000	nM	IC50	J Med Chem (2024) 67: 18606-18628 [PMID:39356741]
ChEMBL	Inhibition of BRD4 BD1 (unknown origin) by Alphascreen assay	B	5.44	pIC50	3670	nM	IC50	J Med Chem (2024) 67: 18606-18628 [PMID:39356741]
ChEMBL	Inhibition of BRD4 bromodomain 1 (unknown origin) using H4K5Ac/K8Ac/K12Ac/K16Ac biotinylated peptide as substrate incubated for 30 mins by HTRF assay	B	6.63	pIC50	231.9	nM	IC50	J Med Chem (2024) 67: 18606-18628 [PMID:39356741]
bromodomain containing 9/Bromodomain-containing protein 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108640] [GtoPdb: 2728] [UniProtKB: Q9H8M2]
ChEMBL	Binding affinity to His6-tagged human BRD9 bromodomain (14 to 134 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by ITC analysis	B	5.58	pKd	2610	nM	Kd	J Med Chem (2022) 65: 785-810 [PMID:34962793]
bromodomain testis associated/Bromodomain testis-specific protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21]
ChEMBL	Binding affinity to His6-tagged human BRDT bromodomain-1 (21 to 137 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by ITC analysis	B	5.95	pKd	1120	nM	Kd	J Med Chem (2022) 65: 785-810 [PMID:34962793]
CREB binding lysine acetyltransferase/CREB-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793]
GtoPdb	Binding affinity for recombinant hCBP bromodomain determined by isothermal titration calorimetry (ITC).	-	7.85	pKd	14	nM	Kd	J Med Chem (2022) 65: 785-810 [PMID:34962793]
ChEMBL	Binding affinity to His6-tagged human CBP bromodomain (1081 to 1197 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by ITC analysis	B	7.85	pKd	14	nM	Kd	J Med Chem (2022) 65: 785-810 [PMID:34962793]
ChEMBL	Binding affinity to CBP (unknown origin) by SPR method	B	8.77	pKd	1.7	nM	Kd	J Med Chem (2024) 67: 6952-6986 [PMID:38649304]
GtoPdb	Binding affinity for hCBP bromodomain determined by surface plasmon resonance (SPR).	-	8.77	pKd	1.7	nM	Kd	Cancer Discov (2021) 11: 1118-1137 [PMID:33431496]
ChEMBL	Binding affinity to CBP (unknown origin) by SPR assay	B	8.89	pKd	1.3	nM	Kd	J Med Chem (2024) 67: 5351-5372 [PMID:38530938]
ChEMBL	Binding affinity to CBP (unknown origin) assessed as dissociation constant by SPR analysis	B	8.89	pKd	1.3	nM	Kd	J Med Chem (2024) 67: 5275-5304 [PMID:38477974]
ChEMBL	Binding affinity to CBP BD (unknown origin) incubated for 2.5 hrs by Alphascreen assay	B	7.04	pIC50	91.4	nM	IC50	J Med Chem (2024) 67: 6952-6986 [PMID:38649304]
ChEMBL	Inhibition of C-terminal biotinylated tetra-acetylated histone peptide H4 binding to His6-fused human CBP bromodomain (R1081 to G1197 residues) incubated for 1 hrs by HTRF assay	B	8.52	pIC50	3	nM	IC50	J Med Chem (2024) 67: 9194-9213 [PMID:38829718]
ChEMBL	Inhibition of His6-tagged human CBP bromodomain (1081 to 1197 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins by HTRF assay	B	8.69	pIC50	2.05	nM	IC50	J Med Chem (2022) 65: 785-810 [PMID:34962793]
EP300 lysine acetyltransferase/Histone acetyltransferase p300 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3784] [GtoPdb: 2735] [UniProtKB: Q09472]
ChEMBL	Binding affinity to p300 (unknown origin) by SPR assay	B	8.77	pKd	1.7	nM	Kd	J Med Chem (2024) 67: 5351-5372 [PMID:38530938]
ChEMBL	Binding affinity to p300 (unknown origin) assessed as dissociation constant by SPR analysis	B	8.77	pKd	1.7	nM	Kd	J Med Chem (2024) 67: 5275-5304 [PMID:38477974]
GtoPdb	Binding affinity for human p300 bromodomain determined by surface plasmon resonance (SPR)	-	8.77	pKd	1.7	nM	Kd	Cancer Discov (2021) 11: 1118-1137 [PMID:33431496]
ChEMBL	Binding affinity to p300 (unknown origin) by SPR method	B	8.89	pKd	1.3	nM	Kd	J Med Chem (2024) 67: 6952-6986 [PMID:38649304]
ChEMBL	Inhibition of p300 (unknown origin)	B	7.19	pIC50	64	nM	IC50	Bioorg Med Chem Lett (2024) 104: 129742-129742 [PMID:38604299]
GtoPdb	Inhibition of histone binding determined in a cell-based BRET assay.	-	7.72	pIC50	19	nM	IC50	Cancer Discov (2021) 11: 1118-1137 [PMID:33431496]
ChEMBL	Inhibition of C-terminal biotinylated tetra-acetylated histone peptide H4 binding to His6-fused human p300 bromodomain (A1040 to G1161 residues) incubated for 1 hrs by HTRF assay	B	8.3	pIC50	5	nM	IC50	J Med Chem (2024) 67: 9194-9213 [PMID:38829718]
ChEMBL	Inhibition of recombinant p300 bromodomain (unknown origin) using H3(44-60)K56Ac-biotinylated peptide as substrate incubated for 120 mins by AlphaLISA	B	8.35	pIC50	4.5	nM	IC50	J Med Chem (2024) 67: 18606-18628 [PMID:39356741]
cereblon/Protein cereblon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3763008] [GtoPdb: 3086] [UniProtKB: Q96SW2]
ChEMBL	Inhibition of biotinylated thalidomide binding to CRBN (40 to 442 residues) (unknown origin) incubated for 1 hrs by HTRF assay	B	4	pIC50	>100000	nM	IC50	J Med Chem (2024) 67: 9194-9213 [PMID:38829718]

ChEMBL data shown on this page come from version 36:

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]