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Assay Detail

CHEMBL2153950

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

Binding
Displacement of [125I]-Tyr6, His5 from human LHRH1 receptor expressed in HEK 293 cells after 16 to 19 hrs by gamma counter
13
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Rationally designed cyclic analogues of luteinizing hormone-releasing hormone: enhanced enzymatic stability and biological properties.
Laimou D, Katsila T, Matsoukas J, Schally A, Gkountelias K, Liapakis G, Tamvakopoulos C, Tselios T.
Eur J Med Chem (2012) 58 : 237 -247
PubMed 23127987 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 7 - -
IC50 6 6.26 9.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1201199 LEUPROLIDE 4.0 2 9.12
CHEMBL2370110 2 6.17
CHEMBL2370111 2 5.82
CHEMBL2370114 2 5.58
CHEMBL2370113 2 5.54
CHEMBL2370112 2 5.31
CHEMBL1007 GONADORELIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1201199 LEUPROLIDE IC50 = 0.7586 nM 9.12
CHEMBL2370110 IC50 = 676.08 nM 6.17
CHEMBL2370111 IC50 = 1513.56 nM 5.82
CHEMBL2370114 IC50 = 2630.27 nM 5.58
CHEMBL2370113 IC50 = 2884.03 nM 5.54
CHEMBL2370112 IC50 = 4897.79 nM 5.31
CHEMBL1007 GONADORELIN Inhibition - % -
CHEMBL1201199 LEUPROLIDE Inhibition - % -
CHEMBL2370110 Inhibition - % -
CHEMBL2370111 Inhibition - % -
CHEMBL2370112 Inhibition - % -
CHEMBL2370113 Inhibition - % -
CHEMBL2370114 Inhibition - % -