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Assay Detail

CHEMBL5665196

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

Binding
Antagonist activity against GPR65 D153A mutant (unknown origin) transfected in human HEK293T cells incubated for 15 mins by luminescence counter analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
2
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 2 5.55 5.89

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
CHEMBL4524214 1 5.89
CHEMBL1492152 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4524214 EC50 = 1288.25 nM 5.89
CHEMBL1492152 EC50 = 6309.57 nM 5.20