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Assay Detail

CHEMBL815446

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

Binding
Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site.
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vasopressin V1a receptor (CHEMBL2868)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Development of a novel class of cyclic hexapeptide oxytocin antagonists based on a natural product.
Williams PD, Bock MG, Tung RD, Garsky VM, Perlow DS, Erb JM, Lundell GF, Gould NP, Whitter WL, Hoffman JB.
J Med Chem (1992) 35 : 3905 -3918
PubMed 1331448 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.55 6.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL340204 1 6.29
CHEMBL2112250 1 6.12
CHEMBL338308 1 6.10
CHEMBL2112655 1 5.96
CHEMBL127686 1 5.89
CHEMBL405289 1 5.89
CHEMBL338018 1 5.89
CHEMBL419793 1 5.80
CHEMBL126765 1 5.80
CHEMBL338294 1 5.70
CHEMBL2112249 1 5.58
CHEMBL338020 1 5.52
CHEMBL339118 1 5.50
CHEMBL52813 1 5.48
CHEMBL2370623 1 5.46
CHEMBL2112247 1 5.43
CHEMBL2112248 1 5.40
CHEMBL129733 1 5.24
CHEMBL2112654 1 5.14
CHEMBL1790937 1 5.13
CHEMBL2112651 1 4.92
CHEMBL1790938 1 4.85
CHEMBL435021 1 4.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL340204 IC50 = 510.0 nM 6.29
CHEMBL2112250 IC50 = 750.0 nM 6.12
CHEMBL338308 IC50 = 800.0 nM 6.10
CHEMBL2112655 IC50 = 1100.0 nM 5.96
CHEMBL127686 IC50 = 1300.0 nM 5.89
CHEMBL405289 IC50 = 1300.0 nM 5.89
CHEMBL338018 IC50 = 1300.0 nM 5.89
CHEMBL419793 IC50 = 1600.0 nM 5.80
CHEMBL126765 IC50 = 1600.0 nM 5.80
CHEMBL338294 IC50 = 2000.0 nM 5.70
CHEMBL2112249 IC50 = 2600.0 nM 5.58
CHEMBL338020 IC50 = 3000.0 nM 5.52
CHEMBL339118 IC50 = 3200.0 nM 5.50
CHEMBL52813 IC50 = 3300.0 nM 5.48
CHEMBL2370623 IC50 = 3500.0 nM 5.46
CHEMBL2112247 IC50 = 3700.0 nM 5.43
CHEMBL2112248 IC50 = 4000.0 nM 5.40
CHEMBL129733 IC50 = 5700.0 nM 5.24
CHEMBL2112654 IC50 = 7300.0 nM 5.14
CHEMBL1790937 IC50 = 7400.0 nM 5.13
CHEMBL2112651 IC50 = 12000.0 nM 4.92
CHEMBL1790938 IC50 = 14000.0 nM 4.85
CHEMBL435021 IC50 = 32000.0 nM 4.50