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Assay Detail

CHEMBL1780594

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

Binding
Displacement of radiolabeled oxytocin from human oxytocin receptor expressed in CHO cells by scintillation counting
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Oxytocin receptor (CHEMBL2049)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties.
Oost T, Backfisch G, Bhowmik S, van Gaalen MM, Geneste H, Hornberger W, Lubisch W, Netz A, Unger L, Wernet W.
Bioorg Med Chem Lett (2011) 21 : 3828 -3831
PubMed 21605973 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.32 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1779407 1 8.15
CHEMBL1779409 1 7.77
CHEMBL1779410 1 7.70
CHEMBL582857 NELIVAPTAN 2.0 1 7.60
CHEMBL1779406 1 7.55
CHEMBL1779408 1 7.54
CHEMBL1779400 1 7.38
CHEMBL1779404 1 7.35
CHEMBL1779405 1 7.35
CHEMBL1779401 1 7.21
CHEMBL1779420 1 7.05
CHEMBL1779418 1 6.94
CHEMBL1779419 1 6.87
CHEMBL1779417 1 6.77
CHEMBL1779403 1 6.57
CHEMBL1779402 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1779407 Ki = 7.0 nM 8.15
CHEMBL1779409 Ki = 17.0 nM 7.77
CHEMBL1779410 Ki = 20.0 nM 7.70
CHEMBL582857 NELIVAPTAN Ki = 25.0 nM 7.60
CHEMBL1779406 Ki = 28.0 nM 7.55
CHEMBL1779408 Ki = 29.0 nM 7.54
CHEMBL1779400 Ki = 42.0 nM 7.38
CHEMBL1779404 Ki = 45.0 nM 7.35
CHEMBL1779405 Ki = 45.0 nM 7.35
CHEMBL1779401 Ki = 62.0 nM 7.21
CHEMBL1779420 Ki = 89.0 nM 7.05
CHEMBL1779418 Ki = 115.0 nM 6.94
CHEMBL1779419 Ki = 135.0 nM 6.87
CHEMBL1779417 Ki = 170.0 nM 6.77
CHEMBL1779403 Ki = 271.0 nM 6.57
CHEMBL1779402 Ki - -