bromosporine [Ligand Id: 8234] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3133807 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ATPase family AAA domain containing 2/ATPase family AAA domain-containing protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2150837] [GtoPdb: 2719] [UniProtKB: Q6PL18] | ||||||||
| ChEMBL | Binding affinity to human partial length ATAD2A (Q981 to R1108 residues) expressed in Escherichia coli BL21(DE3) cells after 1 hr by competitive binding assay | B | 4.36 | pKd | 44000 | nM | Kd | J Med Chem (2019) 62: 7506-7525 [PMID:31398032] |
| bromodomain adjacent to zinc finger domain 2A/Bromodomain adjacent to zinc finger domain protein 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108642] [GtoPdb: 2721] [UniProtKB: Q9UIF9] | ||||||||
| ChEMBL | Reverse ITC (compound as receptor). Domain start/stop: H1769-Q1872 | B | 5.43 | pKd | 3745.3 | nM | Kd | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| bromodomain and PHD finger containing 3/Bromodomain and PHD finger-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108644] [GtoPdb: 2731] [UniProtKB: Q9ULD4] | ||||||||
| ChEMBL | Reverse ITC (compound as receptor). Domain start/stop: L591-P711 | B | 5.06 | pKd | 8620.7 | nM | Kd | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| bromodomain containing 1/Bromodomain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176774] [GtoPdb: 2724] [UniProtKB: O95696] | ||||||||
| ChEMBL | Reverse ITC (compound as receptor). Domain start/stop: E556-A688 | B | 5.78 | pKd | 1652.9 | nM | Kd | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| bromodomain containing 2/Bromodomain-containing protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293289] [GtoPdb: 1944] [UniProtKB: P25440] | ||||||||
| ChEMBL | Reverse ITC (compound as receptor). Domain start/stop: E348-D455 | B | 7.3 | pKd | 50.3 | nM | Kd | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| 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 BRD4 BD1 expressed in Escherichia coli BL21 DE3 assessed as dissociation constant by isothermal titration calorimetry | B | 7.38 | pKd | 42 | nM | Kd | J Med Chem (2020) 63: 3227-3237 [PMID:32091206] |
| ChEMBL | Alphascreen assay. Binding to BRD4A (domain start/stop: N44-E168) by alphascreen assay | B | 6.33 | pIC50 | 468.4 | nM | IC50 | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| ChEMBL | Alphascreen assay. Binding to BRD4A (domain start/stop: N44-E168) by alphascreen assay | B | 6.51 | pIC50 | 310.9 | nM | IC50 | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| ChEMBL | Homogeneous Time Resolved Fluorescence (HTRF) assay. Domain start/stop: N44-E168 | B | 6.94 | pIC50 | 116.1 | nM | IC50 | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| ChEMBL | Alphascreen assay. Binding to BRD4A (domain start/stop: N44-E168) by alphascreen assay | B | 7.08 | pIC50 | 83 | nM | IC50 | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| bromodomain containing 9/Bromodomain-containing protein 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108640] [GtoPdb: 2728] [UniProtKB: Q9H8M2] | ||||||||
| ChEMBL | Binding affinity to human recombinant biotinylated BRD9 compound treated in ammonium acetate buffer by FAC-MS analysis | B | 5.83 | pKd | 1480 | nM | Kd | Medchemcomm (2014) 5: 540-546 |
| ChEMBL | Binding affinity to human recombinant biotinylated BRD9 compound treated in PBS buffer by FAC-MS analysis | B | 5.83 | pKd | 1480 | nM | Kd | Medchemcomm (2014) 5: 540-546 |
| ChEMBL | Binding affinity to recombinant human His-tagged BRD9 (134 to 239 residues) expressed in Escherichia coli BL21 DE3 assessed as dissociation constant by isothermal titration calorimetry | B | 6.94 | pKd | 114 | nM | Kd | J Med Chem (2020) 63: 3227-3237 [PMID:32091206] |
| ChEMBL | Alphascreen assay. Binding to BRD9A (domain start/stop: L14-Q143) by alphascreen assay | B | 6.15 | pIC50 | 701.3 | nM | IC50 | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| ChEMBL | Alphascreen assay. Binding to BRD9A (domain start/stop: L14-Q143) by alphascreen assay | B | 6.52 | pIC50 | 300.2 | nM | IC50 | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| ChEMBL | Inhibition of BRD9 (unknown origin) using H4 peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by Alphascreen assay | B | 6.8 | pIC50 | 160 | nM | IC50 | Bioorg Med Chem (2019) 27: 1391-1404 [PMID:30824168] |
| ChEMBL | Homogeneous Time Resolved Fluorescence (HTRF) assay. Domain start/stop: L14-Q143 | B | 7.33 | pIC50 | 47 | nM | IC50 | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| bromodomain testis associated/Bromodomain testis-specific protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21] | ||||||||
| ChEMBL | Reverse ITC (compound as receptor). Domain start/stop: S257-E382 | B | 6.76 | pKd | 172.1 | nM | Kd | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| ChEMBL | Reverse ITC (compound as receptor). Domain start/stop: N21-E137 | B | 7.4 | pKd | 40.2 | nM | Kd | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| CECR2 histone acetyl-lysine reader/Cat eye syndrome critical region protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108639] [GtoPdb: 2733] [UniProtKB: Q9BXF3] | ||||||||
| ChEMBL | Binding affinity to CECR2 (unknown origin) by ITC analysis | B | 8 | pKd | 10 | nM | Kd | J Med Chem (2020) 63: 5212-5241 [PMID:32321240] |
| ChEMBL | Reverse ITC (compound as receptor). Domain start/stop: P420-D543 | B | 8.1 | pKd | 8 | nM | Kd | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| ChEMBL | Alphascreen assay. Binding to CECR2A (domain start/stop: P420-D543) by alphascreen assay | B | 7.1 | pIC50 | 79.3 | nM | IC50 | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| ChEMBL | Alphascreen assay. Binding to CECR2A (domain start/stop: P420-D543) by alphascreen assay | B | 7.32 | pIC50 | 48.3 | nM | IC50 | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| ChEMBL | Alphascreen assay. Binding to CECR2A (domain start/stop: P420-H538) by alphascreen assay | B | 8.03 | pIC50 | 9.4 | nM | IC50 | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| CREB binding protein/CREB-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793] | ||||||||
| ChEMBL | Alphascreen assay. Binding to CREBBPA (domain start/stop: R1081-G1197) by alphascreen assay | B | 5.61 | pIC50 | 2439.9 | nM | IC50 | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| lysine acetyltransferase 2B/Histone acetyltransferase PCAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5500] [GtoPdb: 2737] [UniProtKB: Q92831] | ||||||||
| ChEMBL | Reverse ITC (compound as receptor). Domain start/stop: G715-D831 | B | 5.32 | pKd | 4761.9 | nM | Kd | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| ChEMBL | Inhibition of PCAF (unknown origin) by fluorometric assay | B | 5.68 | pIC50 | 2100 | nM | IC50 | Bioorg Med Chem (2021) 42: 116266-116266 [PMID:34126285] |
| bromodomain PHD finger transcription factor/Nucleosome-remodeling factor subunit BPTF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3085621] [GtoPdb: 2723] [UniProtKB: Q12830] | ||||||||
| ChEMBL | Reverse ITC (compound as receptor). Domain start/stop: S2791-H2911 | B | 5.72 | pKd | 1886.8 | nM | Kd | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| bromodomain and PHD finger containing 1/Peregrin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3132741] [GtoPdb: 2730] [UniProtKB: P55201] | ||||||||
| ChEMBL | Alphascreen assay. Binding to BRPF1B (domain start/stop: M626-G740) by alphascreen assay | B | 6.85 | pIC50 | 140.7 | nM | IC50 | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| polybromo 1/Protein polybromo-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795184] [GtoPdb: 2738] [UniProtKB: Q86U86] | ||||||||
| ChEMBL | Reverse ITC (compound as receptor). Domain start/stop: S613-D734 | B | 4.85 | pKd | 14224.8 | nM | Kd | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 4/Transcription activator BRG1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3085620] [GtoPdb: 2740] [UniProtKB: P51532] | ||||||||
| ChEMBL | Reverse ITC (compound as receptor). Domain start/stop: L1451-E1580 | B | 4.71 | pKd | 19685 | nM | Kd | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| TATA-box binding protein associated factor 1/Transcription initiation factor TFIID subunit 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3217390] [GtoPdb: 2231] [UniProtKB: P21675] | ||||||||
| ChEMBL | Reverse ITC (compound as receptor). Domain start/stop: R1398-D1524 | B | 5.26 | pKd | 5524.9 | nM | Kd | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| ChEMBL | Binding affinity to TAF1 BD 1 (unknown origin) assessed as dissociation constant | B | 5.3 | pKd | 5000 | nM | Kd | J Med Chem (2022) 65: 4182-4200 [PMID:35191694] |
| ChEMBL | Binding affinity to human TAF1 tandem bromodomain (1373 to 1499 residues) transfected in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetric analysis | B | 6.83 | pKd | 147 | nM | Kd | J Med Chem (2022) 65: 4182-4200 [PMID:35191694] |
| ChEMBL | Binding affinity to TAF1 BD 2 (unknown origin) assessed as dissociation constant | B | 7.77 | pKd | 17 | nM | Kd | J Med Chem (2022) 65: 4182-4200 [PMID:35191694] |
| ChEMBL | Reverse ITC (compound as receptor). Domain start/stop: D1522-D1656 | B | 7.78 | pKd | 16.6 | nM | Kd | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| TATA-box binding protein associated factor 1 like/Transcription initiation factor TFIID subunit 1-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108641] [GtoPdb: 2232] [UniProtKB: Q8IZX4] | ||||||||
| ChEMBL | Reverse ITC (compound as receptor). Domain start/stop: M1401-D1522 | B | 4.6 | pKd | 25000 | nM | Kd | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
| tripartite motif containing 24/Transcription intermediary factor 1-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108638] [GtoPdb: 2252] [UniProtKB: O15164] | ||||||||
| ChEMBL | Reverse ITC (compound as receptor). Domain start/stop: G861-E979 | B | 5.07 | pKd | 8474.6 | nM | Kd | Sci Adv (2016) null: e1600760-null [PMID:27757418] |
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]
