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Assay Detail

CHEMBL685311

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

Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Pituitary gland cell
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Gonadotropin-releasing hormone receptor (CHEMBL3066)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel gonadotropin-releasing hormone antagonists: peptides incorporating modified N omega-cyanoguanidino moieties.
Theobald P, Porter J, Rivier C, Corrigan A, Hook W, Siraganian R, Perrin M, Vale W, Rivier J.
J Med Chem (1991) 34 : 2395 -2402
PubMed 1714956 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 17 9.28 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL414113 1 10.10
CHEMBL386314 1 9.96
CHEMBL2369860 1 9.68
CHEMBL414391 1 9.62
CHEMBL218396 1 9.57
CHEMBL269583 1 9.57
CHEMBL438762 1 9.49
CHEMBL261999 1 9.39
CHEMBL438191 1 9.35
CHEMBL2369851 1 9.32
CHEMBL407482 1 9.00
CHEMBL407023 1 8.92
CHEMBL439359 1 8.92
CHEMBL411586 1 8.89
CHEMBL412802 1 8.77
CHEMBL428837 1 8.68
CHEMBL265522 1 8.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL414113 Kd = 0.08 nM 10.10
CHEMBL386314 Kd = 0.11 nM 9.96
CHEMBL2369860 Kd = 0.21 nM 9.68
CHEMBL414391 Kd = 0.24 nM 9.62
CHEMBL218396 Kd = 0.27 nM 9.57
CHEMBL269583 Kd = 0.27 nM 9.57
CHEMBL438762 Kd = 0.32 nM 9.49
CHEMBL261999 Kd = 0.41 nM 9.39
CHEMBL438191 Kd = 0.45 nM 9.35
CHEMBL2369851 Kd = 0.48 nM 9.32
CHEMBL407482 Kd = 1.0 nM 9.00
CHEMBL407023 Kd = 1.2 nM 8.92
CHEMBL439359 Kd = 1.2 nM 8.92
CHEMBL411586 Kd = 1.3 nM 8.89
CHEMBL412802 Kd = 1.7 nM 8.77
CHEMBL428837 Kd = 2.1 nM 8.68
CHEMBL265522 Kd = 3.3 nM 8.48