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Assay Detail

CHEMBL907382

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

Binding
Displacement of [3H]AVP from rat OT receptor expressed in CHO cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Oxytocin receptor (CHEMBL3996)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
Pena A, Murat B, Trueba M, Ventura MA, Wo NC, Szeto HH, Cheng LL, Stoev S, Guillon G, Manning M.
J Med Chem (2007) 50 : 835 -847
PubMed 17300166 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 6.84 9.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1429 DESMOPRESSIN 4.0 1 9.01
CHEMBL373742 VASOPRESSIN 4.0 1 8.93
CHEMBL375323 1 7.66
CHEMBL219272 1 7.43
CHEMBL412973 1 7.39
CHEMBL375188 1 7.26
CHEMBL412972 1 7.19
CHEMBL375325 1 6.90
CHEMBL385068 1 6.89
CHEMBL373968 1 6.87
CHEMBL385739 1 6.71
CHEMBL412742 1 6.37
CHEMBL265859 1 6.32
CHEMBL263090 1 6.26
CHEMBL221485 1 6.23
CHEMBL221436 1 6.08
CHEMBL375096 1 6.00
CHEMBL375187 1 5.92
CHEMBL265858 1 5.84
CHEMBL375324 1 5.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1429 DESMOPRESSIN Ki = 0.97 nM 9.01
CHEMBL373742 VASOPRESSIN Ki = 1.17 nM 8.93
CHEMBL375323 Ki = 22.0 nM 7.66
CHEMBL219272 Ki = 37.0 nM 7.43
CHEMBL412973 Ki = 41.0 nM 7.39
CHEMBL375188 Ki = 55.0 nM 7.26
CHEMBL412972 Ki = 64.0 nM 7.19
CHEMBL375325 Ki = 125.0 nM 6.90
CHEMBL385068 Ki = 130.0 nM 6.89
CHEMBL373968 Ki = 134.0 nM 6.87
CHEMBL385739 Ki = 195.0 nM 6.71
CHEMBL412742 Ki = 430.0 nM 6.37
CHEMBL265859 Ki = 481.0 nM 6.32
CHEMBL263090 Ki = 550.0 nM 6.26
CHEMBL221485 Ki = 590.0 nM 6.23
CHEMBL221436 Ki = 826.0 nM 6.08
CHEMBL375096 Ki = 997.0 nM 6.00
CHEMBL375187 Ki = 1200.0 nM 5.92
CHEMBL265858 Ki = 1430.0 nM 5.84
CHEMBL375324 Ki = 3550.0 nM 5.45