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] |
| 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 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]
