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Assay Detail

CHEMBL5665149

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Positive allosteric modulator activity at GPR68 expressed in human HEK293T cells assessed as proton-mediated calcium release at 10 uM incubated for 10 mins by Fluo-4 Direct calcium dye based FLIPR assay (Rvb = 6.78 +/- 0.02 No_unit)
3
Total Activities
3
Compounds Tested
1
Activity Types
2
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Ovarian cancer G-protein coupled receptor 1 (CHEMBL3713916)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65.
Huang XP, Karpiak J, Kroeze WK, Zhu H, Chen X, Moy SS, Saddoris KA, Nikolova VD, Farrell MS, Wang S, Mangano TJ, Deshpande DA, Jiang A, Penn RB, Jin J, Koller BH, Kenakin T, Shoichet BK, Roth BL.
Nature (2015) 527 : 477 -483
PubMed 26550826 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 6.87 6.94

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - EFO:0009386
EFO_TERM EFO_TERM - central nervous system disease

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5665399 1 6.94
CHEMBL4460070 ZINC32547799 1 6.85
CHEMBL4548689 Ogerin 1 6.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5665399 EC50 = 114.82 nM 6.94
CHEMBL4460070 ZINC32547799 EC50 = 141.25 nM 6.85
CHEMBL4548689 Ogerin EC50 = 147.91 nM 6.83