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 |
|---|---|---|---|---|---|---|---|---|
| apelin receptor/Apelin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1628481] [GtoPdb: 36] [UniProtKB: P35414] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: APLNR | F | 5.65 | pEC50 | 2247.36 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2 | F | 5.24 | pEC50 | 5806.46 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| C3a receptor/C3a anaphylatoxin chemotactic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4761] [GtoPdb: 31] [UniProtKB: Q16581] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: C3AR1 | F | 5 | pIC50 | >10000 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| C5a1 receptor/C5a anaphylatoxin chemotactic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2373] [GtoPdb: 32] [UniProtKB: P21730] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: C5AR1 | F | 5 | pIC50 | >10000 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| C5a2 receptor/C5a anaphylatoxin chemotactic receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523478] [GtoPdb: 33] [UniProtKB: Q9P296] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: C5AR2 | F | 5 | pIC50 | >10000 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| CX3CR1/C-X3-C chemokine receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4843] [GtoPdb: 74] [UniProtKB: P49238] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: CX3CR1 | F | 5 | pIC50 | >10000 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| GLP-1 receptor/Glucagon-like peptide 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1784] [GtoPdb: 249] [UniProtKB: P43220] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GLP1R | F | 5.53 | pEC50 | 2949.46 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| GPR119/Glucose-dependent insulinotropic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5652] [GtoPdb: 126] [UniProtKB: Q8TDV5] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR119 | F | 5.62 | pEC50 | 2393.89 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| FFA4 receptor/G-protein coupled receptor 120 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: FFAR4 | F | 5.54 | pEC50 | 2905.57 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| 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 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]
