Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL817099

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

Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL ↗
163
Total Activities
159
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vasopressin V2 receptor (CHEMBL3766) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Nanomolar-affinity, non-peptide oxytocin receptor antagonists.
Evans BE, Lundell GF, Gilbert KF, Bock MG, Rittle KE, Carroll LA, Williams PD, Pawluczyk JM, Leighton JL, Young MB.
J Med Chem (1993) 36 : 3993 -4005
PubMed 8258821 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 163 5.32 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL131477 — — 1 6.55
CHEMBL339524 — — 1 6.35
CHEMBL338711 — — 1 6.31
CHEMBL337889 — — 1 6.27
CHEMBL433662 — — 1 6.24
CHEMBL338921 — — 1 6.21
CHEMBL339756 — — 1 6.19
CHEMBL130891 — — 1 6.18
CHEMBL339768 — — 1 6.13
CHEMBL336082 — — 1 6.09
CHEMBL341049 — — 1 6.03
CHEMBL128258 — — 1 5.96
CHEMBL339498 — — 1 5.96
CHEMBL128749 — — 1 5.89
CHEMBL341289 — — 3 5.85
CHEMBL338951 — — 1 5.82
CHEMBL265073 — — 1 5.77
CHEMBL338984 — — 1 5.77
CHEMBL435019 — — 1 5.77
CHEMBL128219 — — 1 5.75
CHEMBL340388 — — 1 5.72
CHEMBL338576 — — 1 5.72
CHEMBL338383 — — 1 5.68
CHEMBL130905 — — 1 5.68
CHEMBL128712 — — 1 5.68
CHEMBL132389 — — 1 5.66
CHEMBL2112666 — — 1 5.62
CHEMBL405016 — — 1 5.62
CHEMBL436189 — — 1 5.60
CHEMBL337221 — — 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL131477 — IC50 = 280.0 nM 6.55
CHEMBL339524 — IC50 = 450.0 nM 6.35
CHEMBL338711 — IC50 = 490.0 nM 6.31
CHEMBL337889 — IC50 = 540.0 nM 6.27
CHEMBL433662 — IC50 = 570.0 nM 6.24
CHEMBL338921 — IC50 = 620.0 nM 6.21
CHEMBL339756 — IC50 = 650.0 nM 6.19
CHEMBL130891 — IC50 = 660.0 nM 6.18
CHEMBL339768 — IC50 = 740.0 nM 6.13
CHEMBL336082 — IC50 = 810.0 nM 6.09
CHEMBL341049 — IC50 = 940.0 nM 6.03
CHEMBL339498 — IC50 = 1100.0 nM 5.96
CHEMBL128258 — IC50 = 1100.0 nM 5.96
CHEMBL128749 — IC50 = 1300.0 nM 5.89
CHEMBL341289 — IC50 = 1400.0 nM 5.85
CHEMBL338951 — IC50 = 1500.0 nM 5.82
CHEMBL341289 — IC50 = 1500.0 nM 5.82
CHEMBL338984 — IC50 = 1700.0 nM 5.77
CHEMBL435019 — IC50 = 1700.0 nM 5.77
CHEMBL265073 — IC50 = 1700.0 nM 5.77
CHEMBL128219 — IC50 = 1800.0 nM 5.75
CHEMBL340388 — IC50 = 1900.0 nM 5.72
CHEMBL338576 — IC50 = 1900.0 nM 5.72
CHEMBL341289 — IC50 = 2000.0 nM 5.70
CHEMBL338383 — IC50 = 2100.0 nM 5.68
CHEMBL130905 — IC50 = 2100.0 nM 5.68
CHEMBL128712 — IC50 = 2100.0 nM 5.68
CHEMBL132389 — IC50 = 2200.0 nM 5.66
CHEMBL2112666 — IC50 = 2400.0 nM 5.62
CHEMBL405016 — IC50 = 2400.0 nM 5.62
CHEMBL436189 — IC50 = 2500.0 nM 5.60
CHEMBL337221 — IC50 = 2500.0 nM 5.60
CHEMBL130993 — IC50 = 2600.0 nM 5.58
CHEMBL339132 — IC50 = 2700.0 nM 5.57
CHEMBL339497 — IC50 = 2900.0 nM 5.54
CHEMBL337888 — IC50 = 3000.0 nM 5.52
CHEMBL2112663 — IC50 = 3000.0 nM 5.52
CHEMBL128652 — IC50 = 3000.0 nM 5.52
CHEMBL130848 — IC50 = 3000.0 nM 5.52
CHEMBL132211 — IC50 = 3000.0 nM 5.52
CHEMBL128383 — IC50 = 3200.0 nM 5.50
CHEMBL339497 — IC50 = 3300.0 nM 5.48
CHEMBL419973 — IC50 = 3400.0 nM 5.47
CHEMBL130887 — IC50 = 3600.0 nM 5.44
CHEMBL129983 — IC50 = 3800.0 nM 5.42
CHEMBL338548 — IC50 = 4100.0 nM 5.39
CHEMBL128489 — IC50 = 4200.0 nM 5.38
CHEMBL449399 — IC50 = 4400.0 nM 5.36
CHEMBL131551 — IC50 = 4500.0 nM 5.35
CHEMBL128423 — IC50 = 4700.0 nM 5.33