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Assay Detail

CHEMBL687311

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

Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis and structure-activity relationships of 1-arylmethyl-3-(1-methyl-2-amino)ethyl-5-aryl-6-methyluracils as antagonists of the human GnRH Receptor.
Tucci FC, Zhu YF, Guo Z, Gross TD, Connors PJ, Struthers RS, Reinhart GJ, Saunders J, Chen C.
Bioorg Med Chem Lett (2003) 13 : 3317 -3322
PubMed 12951117 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 6.51 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL111820 1 8.30
CHEMBL23730 1 7.70
CHEMBL112559 1 7.70
CHEMBL326804 1 7.70
CHEMBL23830 1 7.47
CHEMBL23321 1 7.16
CHEMBL23237 1 7.12
CHEMBL111933 1 7.07
CHEMBL111980 1 7.05
CHEMBL113183 1 6.82
CHEMBL113068 1 6.72
CHEMBL110052 1 6.60
CHEMBL114399 1 6.55
CHEMBL23256 1 6.50
CHEMBL432262 1 6.43
CHEMBL282707 1 6.40
CHEMBL112188 1 6.37
CHEMBL112461 1 6.26
CHEMBL325233 1 6.23
CHEMBL331592 1 6.14
CHEMBL114619 1 6.11
CHEMBL112881 1 6.02
CHEMBL112131 1 5.92
CHEMBL114183 1 5.80
CHEMBL419212 1 5.75
CHEMBL112730 1 5.70
CHEMBL112625 1 5.16
CHEMBL326885 1 5.08
CHEMBL114370 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL111820 Ki = 5.0 nM 8.30
CHEMBL23730 Ki = 20.0 nM 7.70
CHEMBL112559 Ki = 20.0 nM 7.70
CHEMBL326804 Ki = 20.0 nM 7.70
CHEMBL23830 Ki = 34.0 nM 7.47
CHEMBL23321 Ki = 70.0 nM 7.16
CHEMBL23237 Ki = 75.0 nM 7.12
CHEMBL111933 Ki = 85.0 nM 7.07
CHEMBL111980 Ki = 90.0 nM 7.05
CHEMBL113183 Ki = 150.0 nM 6.82
CHEMBL113068 Ki = 190.0 nM 6.72
CHEMBL110052 Ki = 250.0 nM 6.60
CHEMBL114399 Ki = 280.0 nM 6.55
CHEMBL23256 Ki = 320.0 nM 6.50
CHEMBL432262 Ki = 370.0 nM 6.43
CHEMBL282707 Ki = 400.0 nM 6.40
CHEMBL112188 Ki = 430.0 nM 6.37
CHEMBL112461 Ki = 550.0 nM 6.26
CHEMBL325233 Ki = 590.0 nM 6.23
CHEMBL331592 Ki = 720.0 nM 6.14
CHEMBL114619 Ki = 780.0 nM 6.11
CHEMBL112881 Ki = 950.0 nM 6.02
CHEMBL112131 Ki = 1200.0 nM 5.92
CHEMBL114183 Ki = 1600.0 nM 5.80
CHEMBL419212 Ki = 1800.0 nM 5.75
CHEMBL112730 Ki = 2000.0 nM 5.70
CHEMBL112625 Ki = 7000.0 nM 5.16
CHEMBL326885 Ki = 8300.0 nM 5.08
CHEMBL114370 Ki = 15000.0 nM 4.82