PCO371 [Ligand Id: 12788] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3976807 (Pc-0371, Pco-371, Pco371, PCO371) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| PTH1 receptor/Parathyroid hormone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1793] [GtoPdb: 331] [UniProtKB: Q03431] | ||||||||
| ChEMBL | Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA | F | 5.39 | pEC50 | 4100 | nM | EC50 | J Med Chem (2020) 63: 5089-5099 [PMID:32022560] |
| GtoPdb | - | - | 5.39 | pEC50 | 4100 | nM | EC50 | J Med Chem (2020) 63: 5089-5099 [PMID:32022560] |
| PTH1 receptor/Parathyroid hormone receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6038] [GtoPdb: 331] [UniProtKB: P25961] | ||||||||
| ChEMBL | cAMP Assay: Instead of HKRK-B7 cells, LLC-PK46_RATO_PTH1R cells overexpressing rat PTH1R, which were established at Chugai Pharmaceutical, were used to take measurements in a similar manner to Test Example 1: HKRK-B7 or LLC-PK1 cells were seeded into a 96-well plate at 1×105 cells/well and incubated overnight. On the following day, 50 μl of cAMP assay buffer (DMEM, 2 mM IBMX, 0.2 mg/ml bovine serum albumin, 35 mM Hepes-NaOH, pH 7.4) containing human PTH(1-34) or each compound was added and the plate was placed in a 37° C. incubator. The cells were incubated for 20 minutes. After removing the medium, the cells were washed with 100 μl of cAMP assay buffer once. The plate was placed on dry ice powder to freeze the cells and then removed from the dry ice. The cells were lysed with 40 μl of 50 mM HCl and frozen again on dry ice. The amount of intracellular cAMP produced was measured using a commercially available cAMP EIA kit (Biotrack cAMP EIA system, GE health care). | F | 5.62 | pEC50 | 2400 | nM | EC50 | US-9428505-B2. Hydantoin derivative (2016) |
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]
