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Assay Detail

CHEMBL4430600

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

Functional
Antagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Gonadotropin-releasing hormone receptor (CHEMBL1855)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist.
Kim SM, Lee M, Lee SY, Park E, Lee SM, Kim EJ, Han MY, Yoo T, Ann J, Yoon S, Lee J, Lee J.
J Med Chem (2016) 59 : 9150 -9172
PubMed 27608177 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.10 9.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4449332 1 9.12
CHEMBL4593521 1 9.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4449332 IC50 = 0.76 nM 9.12
CHEMBL4593521 IC50 = 0.86 nM 9.07