TTA-A2 [Ligand Id: 7724] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1684954 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1692-1696 [PMID:21316226] |
| ChEMBL | Displacement of [3S]MK499 from human ERG in HEK293 cells | B | 5 | pIC50 | >10000 | nM | IC50 | ACS Med Chem Lett (2010) 1: 504-509 [PMID:24900239] |
| Cav2.3/Voltage-dependent R-type calcium channel subunit alpha-1E in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1687682] [GtoPdb: 534] [UniProtKB: Q15878] | ||||||||
| ChEMBL | Inhibition of R-type Cav2.3 at -80 mV holding potential by tandard voltage-clamp electrophysiology assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1692-1696 [PMID:21316226] |
| Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936] | ||||||||
| ChEMBL | Inhibition of L-type Cav1.2 at -80 mV holding potential by tandard voltage-clamp electrophysiology assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1692-1696 [PMID:21316226] |
| Cav2.2/Voltage-gated N-type calcium channel alpha-1B subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4478] [GtoPdb: 533] [UniProtKB: Q00975] | ||||||||
| ChEMBL | Inhibition of N-type Cav2.2 at -80 mV holding potential by tandard voltage-clamp electrophysiology assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1692-1696 [PMID:21316226] |
| Cav2.1/Voltage-gated P/Q-type calcium channel alpha-1A subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4266] [GtoPdb: 532] [UniProtKB: O00555] | ||||||||
| ChEMBL | Inhibition of P/Q-type Cav2.1 at -80 mV holding potential by tandard voltage-clamp electrophysiology assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1692-1696 [PMID:21316226] |
| Cav3.1/Voltage-gated T-type calcium channel alpha-1G subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4641] [GtoPdb: 535] [UniProtKB: O43497] | ||||||||
| GtoPdb | - | - | 7 | pIC50 | - | - | - | Pain (2013) 154: 283-93 [PMID:23257507] |
| ChEMBL | Inhibition of Cav3.1 alpha1G at -80 mV holding potential by tandard voltage-clamp electrophysiology assay | B | 7.05 | pIC50 | 89 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1692-1696 [PMID:21316226] |
| Cav3.2/Voltage-gated T-type calcium channel alpha-1H subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1859] [GtoPdb: 536] [UniProtKB: O95180] | ||||||||
| ChEMBL | Inhibition of Cav3.2 alpha1H at -80 mV holding potential by tandard voltage-clamp electrophysiology assay | B | 7.04 | pIC50 | 92 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1692-1696 [PMID:21316226] |
| ChEMBL | Inhibition of human Cav3.2 T-type Ca2+ channel expressed in HEK293 cells assessed as effect on T-currents in response to -20 mV test pulse at -80 mV holding potential by whole cell patch-clamp assay | B | 7.04 | pIC50 | 92 | nM | IC50 | Eur J Med Chem (2022) 243: 114716-114716 [PMID:36075145] |
| GtoPdb | - | - | 8 | pIC50 | - | - | - | Pain (2013) 154: 283-93 [PMID:23257507] |
| Cav3.3/Voltage-gated T-type calcium channel alpha-1I subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5558] [GtoPdb: 537] [UniProtKB: Q9P0X4] | ||||||||
| ChEMBL | Binding affinity to Cav3.3 alpha1i | B | 8.92 | pKi | 1.2 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1692-1696 [PMID:21316226] |
| ChEMBL | Antagonist activity at Cav3.3 alpha1i expressed in HEK293 cells at -80 mV by standard voltage-clamp electrophysiology assay | F | 7.01 | pIC50 | 98 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1692-1696 [PMID:21316226] |
| GtoPdb | - | - | 7.5 | pIC50 | - | - | - | Pain (2013) 154: 283-93 [PMID:23257507] |
| ChEMBL | Antagonist activity at Cav3.3 alpha1i expressed in HEK293 cells at -100 mV by standard voltage-clamp electrophysiology assay | F | 8.43 | pIC50 | 3.7 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1692-1696 [PMID:21316226] |
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]
