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Assay Detail

CHEMBL712508

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

Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Nonpeptide luteinizing hormone-releasing hormone antagonists derived from erythromycin A: design, synthesis, and biological activity of cladinose replacement analogues.
Randolph JT, Waid P, Nichols C, Sauer D, Haviv F, Diaz G, Bammert G, Besecke LM, Segreti JA, Mohning KM, Bush EN, Wegner CD, Greer J.
J Med Chem (2004) 47 : 1085 -1097
PubMed 14971889 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 7.83 9.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12282 1 9.97
CHEMBL273440 1 9.63
CHEMBL303274 1 9.17
CHEMBL275935 1 9.16
CHEMBL273275 1 8.93
CHEMBL273466 1 8.67
CHEMBL275467 1 8.54
CHEMBL273535 1 8.54
CHEMBL273387 1 8.35
CHEMBL429949 1 8.28
CHEMBL412634 1 8.20
CHEMBL267568 1 8.10
CHEMBL273536 1 8.05
CHEMBL268489 1 7.85
CHEMBL430312 1 7.74
CHEMBL428008 1 7.30
CHEMBL12666 1 6.95
CHEMBL275521 1 6.92
CHEMBL268491 1 6.85
CHEMBL12589 1 6.66
CHEMBL275251 1 6.37
CHEMBL276217 1 6.16
CHEMBL416337 1 5.91
CHEMBL12265 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12282 Ki = 0.1072 nM 9.97
CHEMBL273440 Ki = 0.2344 nM 9.63
CHEMBL303274 Ki = 0.6761 nM 9.17
CHEMBL275935 Ki = 0.6918 nM 9.16
CHEMBL273275 Ki = 1.175 nM 8.93
CHEMBL273466 Ki = 2.138 nM 8.67
CHEMBL275467 Ki = 2.884 nM 8.54
CHEMBL273535 Ki = 2.884 nM 8.54
CHEMBL273387 Ki = 4.467 nM 8.35
CHEMBL429949 Ki = 5.248 nM 8.28
CHEMBL412634 Ki = 6.31 nM 8.20
CHEMBL267568 Ki = 7.943 nM 8.10
CHEMBL273536 Ki = 8.913 nM 8.05
CHEMBL268489 Ki = 14.13 nM 7.85
CHEMBL430312 Ki = 18.2 nM 7.74
CHEMBL428008 Ki = 50.12 nM 7.30
CHEMBL12666 Ki = 112.2 nM 6.95
CHEMBL275521 Ki = 120.23 nM 6.92
CHEMBL268491 Ki = 141.25 nM 6.85
CHEMBL12589 Ki = 218.78 nM 6.66
CHEMBL275251 Ki = 426.58 nM 6.37
CHEMBL276217 Ki = 691.83 nM 6.16
CHEMBL416337 Ki = 1230.27 nM 5.91
CHEMBL12265 Ki = 2511.89 nM 5.60