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ChEMBL ligand: CHEMBL4785363 (Ccs 1477, Ccs1477, CCS-1477, CCS1477, Inobrodib) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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] |
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] |
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] |
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 protein/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] |
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 | 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] |
E1A binding protein p300 in Human [GtoPdb: 2735] [UniProtKB: Q09472] | ||||||||
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] |
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 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]