SHA 68 [Ligand Id: 5813] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL469695 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| NPS receptor/Neuropeptide S receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5162] [GtoPdb: 302] [UniProtKB: Q6W5P4] | ||||||||
| ChEMBL | Binding affinity to human NPSR by radioligand binding assay | B | 7.32 | pKi | 47.86 | nM | Ki | J Med Chem (2021) 64: 4089-4108 [PMID:33733768] |
| ChEMBL | Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as inhibition of NPS-induced calcium mobilization after 10 mins by fluorescence assay | F | 6.38 | pIC50 | 420 | nM | IC50 | J Med Chem (2013) 56: 9045-9056 [PMID:24171469] |
| ChEMBL | Antagonist activity at neuropeptide S receptor (unknown origin) assessed as cAMP level by cell based assay | F | 6.38 | pIC50 | 420 | nM | IC50 | J Med Chem (2013) 56: 9045-9056 [PMID:24171469] |
| ChEMBL | Displacement of [125I]Tyr10-NPS from neuropeptide S receptor (unknown origin) | B | 7.32 | pIC50 | 48 | nM | IC50 | J Med Chem (2013) 56: 9045-9056 [PMID:24171469] |
| ChEMBL | Antagonist activity at neuropeptide S receptor (unknown origin) assessed as intracellular calcium level by cell based assay | F | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2013) 56: 9045-9056 [PMID:24171469] |
| ChEMBL | Displacement of [125I]Tyr10-NPS from human neuropeptide S receptor expressed in CHO cells after 1.5 hrs by liquid scintillation counting | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2013) 56: 9045-9056 [PMID:24171469] |
| ChEMBL | Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as inhibition of NPS-induced ERK activation after 20 mins by HTRF assay | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2013) 56: 9045-9056 [PMID:24171469] |
| ChEMBL | Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as cAMP level after 30 mins by phosphate-buffered saline assay | F | 8.28 | pIC50 | 5.3 | nM | IC50 | J Med Chem (2013) 56: 9045-9056 [PMID:24171469] |
| NPS receptor/Neuropeptide S receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5497] [GtoPdb: 302] [UniProtKB: Q8BZP8] | ||||||||
| ChEMBL | Antagonist activity at mouse Neuropeptide S receptor expressed in HEK293 cells assessed as rightward shift in NPS concentration response curve of intracellular calcium mobilization without affecting maximal effect at 100 nM treated for 24 mins prior to NPS addition measured immediately by Fluo-4AM dye based FLIPR assay | F | 7.82 | pKd | 15.14 | nM | Kd | J Med Chem (2021) 64: 4089-4108 [PMID:33733768] |
| GtoPdb | - | - | 8.1 | pA2 | - | - | - | Peptides (2010) 31: 915-25 [PMID:20172007] |
| NPS receptor in Rat [GtoPdb: 302] [UniProtKB: P0C0L6] | ||||||||
| GtoPdb | - | - | 7.6 | pA2 | - | - | - | Peptides (2012) 34: 404-11 [PMID:22342393] |
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]
