dimethyl shikonin oxime 5a [Ligand Id: 14059] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL5406411 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| BB3 receptor/Bombesin receptor subtype-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4080] [GtoPdb: 40] [UniProtKB: P32247] | ||||||||
| ChEMBL | Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assay | F | 7.07 | pIC50 | 85.7 | nM | IC50 | J Med Chem (2023) 66: 8011-8029 [PMID:37272653] |
| ChEMBL | Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assay | F | 8.56 | pIC50 | 2.77 | nM | IC50 | J Med Chem (2023) 66: 8011-8029 [PMID:37272653] |
| ChEMBL | Agonist activity at human BB3 transiently expressed in human HEK293T cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay | F | 6.83 | pEC50 | 149.28 | nM | EC50 | J Med Chem (2023) 66: 8011-8029 [PMID:37272653] |
| ChEMBL | Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assay | F | 7.96 | pEC50 | 10.86 | nM | EC50 | J Med Chem (2023) 66: 8011-8029 [PMID:37272653] |
| GtoPdb | - | - | 8.42 | pEC50 | - | - | - | J Med Chem (2023) 66: 8011-8029 [PMID:37272653] |
| ChEMBL | Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay | F | 8.42 | pEC50 | 3.78 | nM | EC50 | J Med Chem (2023) 66: 8011-8029 [PMID:37272653] |
| BB3 receptor/Bombesin receptor subtype-3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075140] [GtoPdb: 40] [UniProtKB: O54798] | ||||||||
| ChEMBL | Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assay | F | 7.48 | pIC50 | 33.34 | nM | IC50 | J Med Chem (2023) 66: 8011-8029 [PMID:37272653] |
| ChEMBL | Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assay | F | 8.83 | pIC50 | 1.48 | nM | IC50 | J Med Chem (2023) 66: 8011-8029 [PMID:37272653] |
| ChEMBL | Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assay | F | 7.17 | pEC50 | 66.99 | nM | EC50 | J Med Chem (2023) 66: 8011-8029 [PMID:37272653] |
| ChEMBL | Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay | F | 7.26 | pEC50 | 54.7 | nM | EC50 | J Med Chem (2023) 66: 8011-8029 [PMID:37272653] |
| ChEMBL | Agonist activity at endogenous mouse BB3 in mouse B16 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay | F | 9.36 | pEC50 | 0.44 | nM | EC50 | J Med Chem (2023) 66: 8011-8029 [PMID:37272653] |
| BB3 receptor/Bombesin receptor subtype-3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075111] [GtoPdb: 40] [UniProtKB: Q8K418] | ||||||||
| ChEMBL | Agonist activity at rat BB3 transiently expressed in human HEK293T cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay | F | 8.21 | pEC50 | 6.11 | nM | EC50 | J Med Chem (2023) 66: 8011-8029 [PMID:37272653] |
ChEMBL data shown on this page come from version 35:
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]
