Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL853239

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

Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL ↗
62
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Novel analogues of degarelix incorporating hydroxy-, methoxy-, and pegylated-urea moieties at positions 3, 5, 6 and the N-terminus. Part III.
Samant MP, Hong DJ, Croston G, Rivier C, Rivier J.
J Med Chem (2006) 49 : 3536 -3543
PubMed 16759096 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 62 8.77 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL435141 — — 2 9.29
CHEMBL415606 DEGARELIX 4.0 2 9.24
CHEMBL407661 — — 2 9.22
CHEMBL262747 ACYLINE 2.0 2 9.16
CHEMBL434380 — — 2 9.15
CHEMBL427976 — — 2 9.10
CHEMBL429527 — — 2 9.07
CHEMBL438239 — — 2 9.06
CHEMBL219061 — — 2 9.04
CHEMBL409044 — — 2 8.97
CHEMBL409043 — — 2 8.95
CHEMBL262180 — — 2 8.86
CHEMBL263691 — — 2 8.84
CHEMBL376654 — — 2 8.83
CHEMBL219562 — — 2 8.82
CHEMBL376728 — — 2 8.79
CHEMBL413688 — — 2 8.78
CHEMBL411337 — — 2 8.77
CHEMBL438629 — — 2 8.69
CHEMBL264781 — — 2 8.67
CHEMBL268450 — — 2 8.59
CHEMBL425813 — — 2 8.57
CHEMBL268813 — — 2 8.53
CHEMBL264779 — — 2 8.53
CHEMBL219532 — — 2 8.50
CHEMBL411381 — — 2 8.50
CHEMBL428484 — — 2 8.46
CHEMBL376466 — — 2 8.38
CHEMBL411749 — — 2 8.34
CHEMBL429016 — — 2 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL435141 — IC50 = 0.5129 nM 9.29
CHEMBL435141 — IC50 = 0.51 nM 9.29
CHEMBL415606 DEGARELIX IC50 = 0.58 nM 9.24
CHEMBL415606 DEGARELIX IC50 = 0.5754 nM 9.24
CHEMBL407661 — IC50 = 0.6 nM 9.22
CHEMBL407661 — IC50 = 0.6026 nM 9.22
CHEMBL262747 ACYLINE IC50 = 0.69 nM 9.16
CHEMBL262747 ACYLINE IC50 = 0.6918 nM 9.16
CHEMBL434380 — IC50 = 0.7 nM 9.15
CHEMBL434380 — IC50 = 0.7079 nM 9.15
CHEMBL427976 — IC50 = 0.8 nM 9.10
CHEMBL427976 — IC50 = 0.8128 nM 9.09
CHEMBL429527 — IC50 = 0.8511 nM 9.07
CHEMBL429527 — IC50 = 0.86 nM 9.07
CHEMBL438239 — IC50 = 0.88 nM 9.06
CHEMBL438239 — IC50 = 0.871 nM 9.06
CHEMBL219061 — IC50 = 0.912 nM 9.04
CHEMBL219061 — IC50 = 0.91 nM 9.04
CHEMBL409044 — IC50 = 1.06 nM 8.97
CHEMBL409044 — IC50 = 1.072 nM 8.97
CHEMBL409043 — IC50 = 1.12 nM 8.95
CHEMBL409043 — IC50 = 1.122 nM 8.95
CHEMBL262180 — IC50 = 1.37 nM 8.86
CHEMBL262180 — IC50 = 1.38 nM 8.86
CHEMBL263691 — IC50 = 1.46 nM 8.84
CHEMBL263691 — IC50 = 1.479 nM 8.83
CHEMBL376654 — IC50 = 1.479 nM 8.83
CHEMBL376654 — IC50 = 1.49 nM 8.83
CHEMBL219562 — IC50 = 1.514 nM 8.82
CHEMBL219562 — IC50 = 1.53 nM 8.81
CHEMBL376728 — IC50 = 1.622 nM 8.79
CHEMBL376728 — IC50 = 1.61 nM 8.79
CHEMBL413688 — IC50 = 1.66 nM 8.78
CHEMBL413688 — IC50 = 1.67 nM 8.78
CHEMBL411337 — IC50 = 1.69 nM 8.77
CHEMBL411337 — IC50 = 1.698 nM 8.77
CHEMBL438629 — IC50 = 2.042 nM 8.69
CHEMBL438629 — IC50 = 2.04 nM 8.69
CHEMBL264781 — IC50 = 2.13 nM 8.67
CHEMBL264781 — IC50 = 2.138 nM 8.67
CHEMBL268450 — IC50 = 2.57 nM 8.59
CHEMBL268450 — IC50 = 2.55 nM 8.59
CHEMBL425813 — IC50 = 2.692 nM 8.57
CHEMBL425813 — IC50 = 2.68 nM 8.57
CHEMBL264779 — IC50 = 2.951 nM 8.53
CHEMBL268813 — IC50 = 2.98 nM 8.53
CHEMBL264779 — IC50 = 2.98 nM 8.53
CHEMBL268813 — IC50 = 2.951 nM 8.53
CHEMBL219532 — IC50 = 3.16 nM 8.50
CHEMBL219532 — IC50 = 3.162 nM 8.50