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 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]
