NP118809 [Ligand Id: 7765] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL604710 (MK-6721, MK6721, NMED-160, NP-118809, Z-160, Z160) |
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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: P54289, Q00975, Q02641] | ||||||||
| 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: P54289, Q02641, Q13936] | ||||||||
| 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: P54283, P54290, Q02294] | ||||||||
| 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 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]
