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Assay Detail

CHEMBL760331

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

Functional
Compound was evaluated for its antagonism in CHO cells expressing the human receptor (hPI)
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Quinolones as gonadotropin releasing hormone (GnRH) antagonists: simultaneous optimization of the C(3)-aryl and C(6)-substituents.
Young JR, Huang SX, Chen I, Walsh TF, DeVita RJ, Wyvratt MJ, Goulet MT, Ren N, Lo J, Yang YT, Yudkovitz JB, Cheng K, Smith RG.
Bioorg Med Chem Lett (2000) 10 : 1723 -1727
PubMed 10937733 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.72 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL48192 1 8.66
CHEMBL45883 1 8.30
CHEMBL296321 2 8.30
CHEMBL49230 1 8.19
CHEMBL48165 1 8.15
CHEMBL45784 1 8.11
CHEMBL46177 1 8.07
CHEMBL50283 1 8.05
CHEMBL48674 1 7.80
CHEMBL46312 1 7.64
CHEMBL48249 1 7.28
CHEMBL49293 1 6.65
CHEMBL45501 1 6.64
CHEMBL417189 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL48192 IC50 = 2.2 nM 8.66
CHEMBL45883 IC50 = 5.0 nM 8.30
CHEMBL296321 IC50 = 5.0 nM 8.30
CHEMBL49230 IC50 = 6.5 nM 8.19
CHEMBL48165 IC50 = 7.1 nM 8.15
CHEMBL45784 IC50 = 7.7 nM 8.11
CHEMBL46177 IC50 = 8.5 nM 8.07
CHEMBL50283 IC50 = 9.0 nM 8.05
CHEMBL296321 IC50 = 12.0 nM 7.92
CHEMBL48674 IC50 = 16.0 nM 7.80
CHEMBL46312 IC50 = 23.0 nM 7.64
CHEMBL48249 IC50 = 53.0 nM 7.28
CHEMBL49293 IC50 = 225.0 nM 6.65
CHEMBL45501 IC50 = 227.0 nM 6.64
CHEMBL417189 IC50 = 897.0 nM 6.05