Assay Detail

CHEMBL680412

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Functional

Functional antagonism at GnRH receptor in rat (PI turnover)

ChEMBL ↗

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Target

Gonadotropin-releasing hormone receptor (CHEMBL3066) ↗

Open DB target context

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Gonadotropin-releasing hormone receptor (CHEMBL3066) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Gonadotropin-releasing hormone receptor

CHEMBL3066

Anchored from Assay target.

Protein identity Gonadotropin-releasing hormone receptor

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Functional
Confidence	8 — Homologous single protein target
Curated By	Autocuration

Target

Gonadotropin-releasing hormone receptor (CHEMBL3066) ↗

Type	SINGLE PROTEIN
Organism	Rattus norvegicus

Publication

A potent, nonpeptidyl 1H-quinolone antagonist for the gonadotropin-releasing hormone receptor.

DeVita RJ, Walsh TF, Young JR, Jiang J, Ujjainwalla F, Toupence RB, Parikh M, Huang SX, Fair JA, Goulet MT, Wyvratt MJ, Lo JL, Ren N, Yudkovitz JB, Yang YT, Cheng K, Cui J, Mount G, Rohrer SP, Schaeffer JM, Rhodes L, Drisko JE, McGowan E, MacIntyre DE, Vincent S, Carlin JR, Cameron J, Smith RG.
J Med Chem (2001) 44 : 917 -922
PubMed 11300873 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	7.09	7.09

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL120432	—	—	1	7.09

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL120432	—	IC50	=	81.0	nM	7.09