NPS 2143 [Ligand Id: 716] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL180672 (NPS-2143, SB-262470) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
| ChEMBL | Inhibition of beta2 adrenergic receptor | B | 8.37 | pIC50 | 4.3 | nM | IC50 | J Med Chem (2009) 52: 6599-6605 [PMID:19821575] |
| CaS receptor/Calcium sensing receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1878] [GtoPdb: 54] [UniProtKB: P41180] | ||||||||
| ChEMBL | Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR | F | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 5478-5482 [PMID:16216508] |
| ChEMBL | Inhibitory concentration was evaluated for in vitro calcilytic activity against human calcium receptor | B | 7.37 | pIC50 | 43 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2537-2540 [PMID:15863312] |
| ChEMBL | Inhibitory concentration against human calcium receptor expressed in HEK 293 cells | B | 7.37 | pIC50 | 43 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1557-1560 [PMID:15745796] |
| ChEMBL | Inhibition of human CaSR expressed in HEK293 cells | B | 7.37 | pIC50 | 43 | nM | IC50 | J Med Chem (2010) 53: 4332-4353 [PMID:20218623] |
| GtoPdb | - | - | 7.4 | pIC50 | - | - | - |
Bioorg Med Chem Lett (2005) 15: 1225-8 [PMID:15686947]; J Pharmacol Exp Ther (2001) 299: 323-31 [PMID:11561095] |
| ChEMBL | Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay | F | 7.59 | pIC50 | 26 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3809-3813 [PMID:20472433] |
| ChEMBL | Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells | F | 7.64 | pIC50 | 23 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3328-3332 [PMID:19442519] |
| ChEMBL | Antagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assay | F | 10.24 | pIC50 | 0.06 | nM | IC50 | J Med Chem (2009) 52: 6599-6605 [PMID:19821575] |
| CaS receptor/Calcium sensing receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2516] [GtoPdb: 54] [UniProtKB: P48442] | ||||||||
| ChEMBL | Inhibition of extracellular calcium-induced inositol triphosphate generation in rat MTC cells expressing calcium-sensing receptor | F | 6.28 | pIC50 | 530 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 5478-5482 [PMID:16216508] |
| ChEMBL | Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation | F | 6.34 | pIC50 | 460 | nM | IC50 | J Med Chem (2006) 49: 5119-5128 [PMID:16913701] |
| DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
| ChEMBL | Inhibition of DAT | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2009) 52: 6599-6605 [PMID:19821575] |
| Extracellular calcium-sensing receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075316] [UniProtKB: P35384] | ||||||||
| ChEMBL | Inhibition of CaSR in bovine parathyroid cells assessed as increase in PTH level | B | 7.39 | pEC50 | 41 | nM | EC50 | J Med Chem (2010) 53: 4332-4353 [PMID:20218623] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibitory concentration against human Kv11.1 ERG potassium channel | B | 6.71 | pIC50 | 194 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1225-1228 [PMID:15686947] |
| ChEMBL | Inhibition of human ERG | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2009) 52: 6599-6605 [PMID:19821575] |
| NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | Inhibition of NET | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2009) 52: 6599-6605 [PMID:19821575] |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | Inhibition of SERT | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2009) 52: 6599-6605 [PMID:19821575] |
| GPRC6 receptor in Mouse [GtoPdb: 55] [UniProtKB: Q8K4Z6] | ||||||||
| GtoPdb | This is an inferred IC50 based on 10µM of the compound inhibiting maximum L-ornithine-induced activation of GPCR6 by approximately 50% (see Fig 1B in reference). | - | 5 | pIC50 | ~10000 | nM | IC50 | Cell Calcium (2009) 46: 323-32 [PMID:19836834] |
| mGlu5 receptor in Rat [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
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]
