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Assay Detail

CHEMBL712505

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

Binding
In vitro binding affinity to human 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 (CHEMBL1855)
Type SINGLE PROTEIN
Organism Homo sapiens

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 6.85 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12282 1 9.48
CHEMBL303274 1 8.73
CHEMBL275935 1 8.25
CHEMBL273440 1 7.82
CHEMBL275467 1 7.73
CHEMBL273387 1 7.65
CHEMBL267568 1 7.44
CHEMBL273275 1 7.42
CHEMBL429949 1 7.31
CHEMBL412634 1 7.18
CHEMBL273536 1 7.10
CHEMBL273466 1 6.94
CHEMBL268489 1 6.67
CHEMBL276217 1 6.56
CHEMBL430312 1 6.25
CHEMBL428008 1 6.20
CHEMBL275521 1 6.10
CHEMBL12666 1 5.79
CHEMBL268491 1 5.69
CHEMBL12589 1 5.69
CHEMBL416337 1 5.33
CHEMBL275251 1 5.25
CHEMBL12265 1 5.00
CHEMBL273535 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12282 Ki = 0.3311 nM 9.48
CHEMBL303274 Ki = 1.862 nM 8.73
CHEMBL275935 Ki = 5.623 nM 8.25
CHEMBL273440 Ki = 15.14 nM 7.82
CHEMBL275467 Ki = 18.62 nM 7.73
CHEMBL273387 Ki = 22.39 nM 7.65
CHEMBL267568 Ki = 36.31 nM 7.44
CHEMBL273275 Ki = 38.02 nM 7.42
CHEMBL429949 Ki = 48.98 nM 7.31
CHEMBL412634 Ki = 66.07 nM 7.18
CHEMBL273536 Ki = 79.43 nM 7.10
CHEMBL273466 Ki = 114.82 nM 6.94
CHEMBL268489 Ki = 213.8 nM 6.67
CHEMBL276217 Ki = 275.42 nM 6.56
CHEMBL430312 Ki = 562.34 nM 6.25
CHEMBL428008 Ki = 630.96 nM 6.20
CHEMBL275521 Ki = 794.33 nM 6.10
CHEMBL12666 Ki = 1621.81 nM 5.79
CHEMBL268491 Ki = 2041.74 nM 5.69
CHEMBL12589 Ki = 2041.74 nM 5.69
CHEMBL416337 Ki = 4677.35 nM 5.33
CHEMBL275251 Ki = 5623.41 nM 5.25
CHEMBL12265 Ki = 10000.0 nM 5.00
CHEMBL273535 Ki < 100.0 nM -