NP118809 [Ligand Id: 7765] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL604710 (MK6721, MK-6721, NMED-160, NP-118809, Z160, Z-160)
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  • Cav2.2/Voltage-dependent L-type calcium channel subunit beta-1/alpha-1B/alpha-2/delta-1 in Rat [ChEMBL: CHEMBL3885653] [GtoPdb: 533] [UniProtKB: P54283P54290Q02294]
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  • Cav2.2/Voltage-gated N-type calcium channel alpha-1B subunit in Human [ChEMBL: CHEMBL4478] [GtoPdb: 533] [UniProtKB: Q00975]
  • Cav2.2 in Rat [GtoPdb: 533] [UniProtKB: Q02294]
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  • Cav3.2/Voltage-gated T-type calcium channel alpha-1H subunit in Human [ChEMBL: CHEMBL1859] [GtoPdb: 536] [UniProtKB: O95180]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Cav2.2/N-type calcium channel alpha-1b/alpha2delta-1/beta-1b in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106160] [GtoPdb: 533] [UniProtKB: P54289Q00975Q02641]
ChEMBL Inhibition of N type calcium channel alpha-1b/alpha-2-delta-1/beta-1b expressed in HEK293 cells at holding potential of -100 mV by whole-cell patch clamp method B 6.96 pIC50 110 nM IC50 Bioorg Med Chem Lett (2010) 20: 1378-1383 [PMID:20117000]
Cav2.2 in Rat [GtoPdb: 533] [UniProtKB: Q02294]
GtoPdb - - 7 pIC50 110 nM IC50 Bioorg Med Chem Lett (2009) 19: 6467-72 [PMID:19815411]
Cav1.2/Voltage-dependent L-type calcium channel alpha1C/alpha2delta/beta1b in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3988638] [GtoPdb: 529] [UniProtKB: P54289Q02641Q13936]
ChEMBL Inhibition of L type calcium channel alpha-1c/alpha-2-delta-1/beta-1b expressed in HEK293 cells in presence of -100 mV holding potential by whole-cell patch clamp method B 4.91 pIC50 12200 nM IC50 Bioorg Med Chem Lett (2010) 20: 1378-1383 [PMID:20117000]
Cav2.2/Voltage-dependent L-type calcium channel subunit beta-1/alpha-1B/alpha-2/delta-1 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885653] [GtoPdb: 533] [UniProtKB: P54283P54290Q02294]
ChEMBL Blocking of rat N-type calcium channel alpha-1B/alpha-2-delta-1/beta-1b activity expressed in HEK293 cells assessed as whole cell current by whole cell patch clamp assay B 6.96 pIC50 110 nM IC50 Bioorg Med Chem Lett (2009) 19: 6467-6472 [PMID:19815411]
GtoPdb - - 7 pIC50 110 nM IC50 Bioorg Med Chem Lett (2009) 19: 6467-72 [PMID:19815411]
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 Cav2.2 in human SH-SY5Y cells assessed as decrease in KCl-induced calcium mobilization measured after 600 secs post compound addition and 300 secs post KCl addition in presence of CaV1 blocker nifedipine by calcium 4 dye-based FLIPR assay B 4.41 pIC50 39000 nM IC50 Bioorg Med Chem (2018) 26: 3046-3059 [PMID:29622412]
Cav2.2 in Rat [GtoPdb: 533] [UniProtKB: Q02294]
GtoPdb - - 7 pIC50 110 nM IC50 Bioorg Med Chem Lett (2009) 19: 6467-72 [PMID:19815411]
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 recombinant human Cav3.2-alpha1 expressed in HEK293T cells assessed as decrease in KCl-induced calcium mobilization measured after 600 secs post compound addition and 300 secs post KCl addition by calcium 4 dye-based FLIPR assay B 4.35 pIC50 45000 nM IC50 Bioorg Med Chem (2018) 26: 3046-3059 [PMID:29622412]

ChEMBL data shown on this page come from version 32:

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]