NNC55-0396 [Ligand Id: 4269] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1551597
  • Cav2.2/Voltage-gated N-type calcium channel alpha-1B subunit in Human [ChEMBL: CHEMBL4478] [GtoPdb: 533] [UniProtKB: Q00975]
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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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  • CatSper1 in Human [GtoPdb: 388] [UniProtKB: Q8NEC5]
  • CatSper1 in Mouse [GtoPdb: 388] [UniProtKB: Q91ZR5]
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  • CatSper2 in Human [GtoPdb: 389] [UniProtKB: Q96P56]
  • CatSper2 in Mouse [GtoPdb: 389] [UniProtKB: A2ARP9]
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  • CatSper3 in Human [GtoPdb: 390] [UniProtKB: Q86XQ3]
  • CatSper3 in Mouse [GtoPdb: 390] [UniProtKB: Q80W99]
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  • CatSper4 in Human [GtoPdb: 391] [UniProtKB: Q7RTX7]
  • CatSper4 in Mouse [GtoPdb: 391] [UniProtKB: Q8BVN3]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 human N type calcium channel Cav2.2 endogenously expressed in SH-SY5Y cells assessed as calcium influx by FRIPR assay B 5.15 pIC50 7000 nM IC50 Bioorg Med Chem (2020) 28: 115655-115655 [PMID:32828422]
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 human T type calcium channel Cav3.2 expressed in HEK-293T cells assessed as calcium influx by FRIPR assay B 5.7 pIC50 2000 nM IC50 Bioorg Med Chem (2020) 28: 115655-115655 [PMID:32828422]
CatSper1 in Human [GtoPdb: 388] [UniProtKB: Q8NEC5]
GtoPdb Patch clamp electrophysiology, kinetic rapid mixing fluometry - 5.7 pIC50 2000 nM IC50 Nature (2011) 471: 387-91 [PMID:21412339];
Nature (2011) 471: 382-6 [PMID:21412338]
CatSper1 in Mouse [GtoPdb: 388] [UniProtKB: Q91ZR5]
GtoPdb Patch clamp electrophysiology - 5.6 pIC50 >2500 nM IC50 Nature (2011) 471: 387-91 [PMID:21412339]
CatSper2 in Human [GtoPdb: 389] [UniProtKB: Q96P56]
GtoPdb Patch clamp electrophysiology and kinetic rapid mixing fluometry. - 5.7 pIC50 2000 nM IC50 Nature (2011) 471: 387-91 [PMID:21412339];
Nature (2011) 471: 382-6 [PMID:21412338]
CatSper2 in Mouse [GtoPdb: 389] [UniProtKB: A2ARP9]
GtoPdb Patch clamp electrophysiology. - 4.6 pIC50 >25000 nM IC50 Nature (2011) 471: 387-91 [PMID:21412339]
CatSper3 in Human [GtoPdb: 390] [UniProtKB: Q86XQ3]
GtoPdb Patch clamp electrophysiology, kinetic rapid mixing fluometry. - 5.7 pIC50 2000 nM IC50 Nature (2011) 471: 387-91 [PMID:21412339];
Nature (2011) 471: 382-6 [PMID:21412338]
CatSper3 in Mouse [GtoPdb: 390] [UniProtKB: Q80W99]
GtoPdb Patch clamp electrophysiology. - 5.6 pIC50 >2500 nM IC50 Nature (2011) 471: 387-91 [PMID:21412339]
CatSper4 in Human [GtoPdb: 391] [UniProtKB: Q7RTX7]
GtoPdb Patch clamp electrophysiology, kinetic rapid mixing fluometry. - 5.7 pIC50 2000 nM IC50 Nature (2011) 471: 387-91 [PMID:21412339];
Nature (2011) 471: 382-6 [PMID:21412338]
CatSper4 in Mouse [GtoPdb: 391] [UniProtKB: Q8BVN3]
GtoPdb Patch clamp electrophysiology. - 5.6 pIC50 >2500 nM IC50 Nature (2011) 471: 387-91 [PMID:21412339]

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]