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 | Binding affinity to BRD4 bromo domain 1 (unknown origin) assessed as dissociation constant by site-directed competition binding assay | B | 7.38 | pKd | 41.8 | nM | Kd | Eur J Med Chem (2023) 249: 115139-115139 [PMID:36736153] |
| 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 | Binding affinity to BRD9 (unknown origin) assessed as dissociation constant by site-directed competition binding assay | B | 7.38 | pKd | 41.7 | nM | Kd | Eur J Med Chem (2023) 249: 115139-115139 [PMID:36736153] |
| 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] |
| ChEMBL | Binding affinity to BRDT bromodomain 1 (unknown origin) assessed as dissociation constant by site-directed competition binding assay | B | 7.4 | pKd | 40.2 | nM | Kd | Eur J Med Chem (2023) 249: 115139-115139 [PMID:36736153] |
| 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 | Binding affinity to CECR2 (unknown origin) assessed as dissociation constant by site-directed competition binding assay | B | 8.1 | pKd | 8 | nM | Kd | Eur J Med Chem (2023) 249: 115139-115139 [PMID:36736153] |
| 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 | Binding affinity to CBP (unknown origin) assessed as dissociation constant by site-directed competition binding assay | B | 5.82 | pKd | 1524 | nM | Kd | Eur J Med Chem (2023) 249: 115139-115139 [PMID:36736153] |
| 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 BAF chromatin remodeling complex subunit ATPase 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 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]
