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Assay Detail

CHEMBL817650

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Binding
Binding affinity against human vasopressin V1b receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
25
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

Vasopressin V1b receptor (CHEMBL1921)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4.
Cheng LL, Stoev S, Manning M, Derick S, Pena A, Mimoun MB, Guillon G.
J Med Chem (2004) 47 : 2375 -2388
PubMed 15084136 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 8.68 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL268306 1 9.64
CHEMBL221436 1 9.54
CHEMBL375324 1 9.43
CHEMBL1429 DESMOPRESSIN 4.0 2 9.43
CHEMBL1790575 1 9.38
CHEMBL2369830 1 9.37
CHEMBL375096 1 9.31
CHEMBL2369836 1 9.28
CHEMBL2369845 1 9.11
CHEMBL2369831 1 9.00
CHEMBL265858 1 8.92
CHEMBL2369829 1 8.92
CHEMBL2369839 1 8.82
CHEMBL2369837 1 8.74
CHEMBL2369838 1 8.70
CHEMBL2369841 1 8.47
CHEMBL2369848 1 8.32
CHEMBL411148 1 8.19
CHEMBL2369840 1 8.11
CHEMBL2369847 1 8.02
CHEMBL2369834 1 7.89
CHEMBL2369842 1 7.83
CHEMBL80877 1 7.64
CHEMBL2369835 1 6.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL268306 Ki = 0.23 nM 9.64
CHEMBL221436 Ki = 0.29 nM 9.54
CHEMBL375324 Ki = 0.37 nM 9.43
CHEMBL1429 DESMOPRESSIN Ki = 0.37 nM 9.43
CHEMBL1790575 Ki = 0.42 nM 9.38
CHEMBL2369830 Ki = 0.43 nM 9.37
CHEMBL375096 Ki = 0.49 nM 9.31
CHEMBL2369836 Ki = 0.52 nM 9.28
CHEMBL2369845 Ki = 0.78 nM 9.11
CHEMBL2369831 Ki = 1.0 nM 9.00
CHEMBL265858 Ki = 1.2 nM 8.92
CHEMBL2369829 Ki = 1.2 nM 8.92
CHEMBL2369839 Ki = 1.5 nM 8.82
CHEMBL2369837 Ki = 1.8 nM 8.74
CHEMBL2369838 Ki = 2.0 nM 8.70
CHEMBL2369841 Ki = 3.4 nM 8.47
CHEMBL2369848 Ki = 4.8 nM 8.32
CHEMBL1429 DESMOPRESSIN Ki = 5.8 nM 8.24
CHEMBL411148 Ki = 6.5 nM 8.19
CHEMBL2369840 Ki = 7.8 nM 8.11
CHEMBL2369847 Ki = 9.5 nM 8.02
CHEMBL2369834 Ki = 12.8 nM 7.89
CHEMBL2369842 Ki = 14.8 nM 7.83
CHEMBL80877 Ki = 22.9 nM 7.64
CHEMBL2369835 Ki = 156.0 nM 6.81