TTA-A2 [Ligand Id: 7724] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL1684954
There should be some charts here, you may need to enable JavaScript!
  • Cav2.3/Voltage-dependent R-type calcium channel subunit alpha-1E in Human [ChEMBL: CHEMBL1687682] [GtoPdb: 534] [UniProtKB: Q15878]
There should be some charts here, you may need to enable JavaScript!
  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
There should be some charts here, you may need to enable JavaScript!
  • Cav2.2/Voltage-gated N-type calcium channel alpha-1B subunit in Human [ChEMBL: CHEMBL4478] [GtoPdb: 533] [UniProtKB: Q00975]
There should be some charts here, you may need to enable JavaScript!
  • Cav2.1/Voltage-gated P/Q-type calcium channel alpha-1A subunit in Human [ChEMBL: CHEMBL4266] [GtoPdb: 532] [UniProtKB: O00555]
There should be some charts here, you may need to enable JavaScript!
  • Cav3.1/Voltage-gated T-type calcium channel alpha-1G subunit in Human [ChEMBL: CHEMBL4641] [GtoPdb: 535] [UniProtKB: O43497]
There should be some charts here, you may need to enable JavaScript!
  • Cav3.2/Voltage-gated T-type calcium channel alpha-1H subunit in Human [ChEMBL: CHEMBL1859] [GtoPdb: 536] [UniProtKB: O95180]
There should be some charts here, you may need to enable JavaScript!
  • Cav3.3/Voltage-gated T-type calcium channel alpha-1I subunit in Human [ChEMBL: CHEMBL5558] [GtoPdb: 537] [UniProtKB: Q9P0X4]
There should be some charts here, you may need to enable JavaScript!
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 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]