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Assay Detail

CHEMBL4676187

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

Binding
Antagonist activity at cynomolgus monkey GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Macaca fascicularis
Cell Type CHO-K1
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery and Characterization of BAY 1214784, an Orally Available Spiroindoline Derivative Acting as a Potent and Selective Antagonist of the Human Gonadotropin-Releasing Hormone Receptor as Proven in a First-In-Human Study in Postmenopausal Women.
Panknin O,Wagenfeld A,Bone W,Bender E,Nowak-Reppel K,Fernández-Montalván AE,Nubbemeyer R,Bäurle S,Ring S,Schmees N,Prien O,Schäfer M,Friedrich C,Zollner TM,Steinmeyer A,Mueller T,Langer G
J Med Chem (2020) 63 : 11854 -11881
PubMed 32960053 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.46 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4537788 BAY-784 1 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4537788 BAY-784 IC50 = 35.0 nM 7.46