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Assay Detail

CHEMBL820170

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

Binding
Displacement of [3H]AVP from AVP-V1a receptor binding site in rat liver
ChEMBL ↗
65
Total Activities
65
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

Orally active, nonpeptide vasopressin V2 receptor antagonists: a novel series of 1-[4-(benzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepines and related compounds.
Ogawa H, Yamashita H, Kondo K, Yamamura Y, Miyamoto H, Kan K, Kitano K, Tanaka M, Nakaya K, Nakamura S, Mori T, Tominaga M, Yabuuchi Y.
J Med Chem (1996) 39 : 3547 -3555
PubMed 8784453 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 65 5.65 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118387 — — 1 7.35
CHEMBL119793 — — 1 7.25
CHEMBL333201 — — 1 7.02
CHEMBL118271 — — 1 6.85
CHEMBL324251 — — 1 6.54
CHEMBL332685 — — 1 6.42
CHEMBL420880 — — 1 6.41
CHEMBL119806 — — 1 6.39
CHEMBL333135 — — 1 6.20
CHEMBL324488 — — 1 6.14
CHEMBL332450 — — 1 6.12
CHEMBL118609 — — 1 6.05
CHEMBL331173 — — 1 6.01
CHEMBL334082 — — 1 6.00
CHEMBL332060 — — 1 5.92
CHEMBL118863 — — 1 5.92
CHEMBL119638 — — 1 5.89
CHEMBL420762 MOZAVAPTAN 4.0 1 5.85
CHEMBL331164 — — 1 5.85
CHEMBL118922 — — 1 5.80
CHEMBL333139 — — 1 5.80
CHEMBL118660 — — 1 5.80
CHEMBL334009 — — 1 5.77
CHEMBL333652 — — 1 5.75
CHEMBL118878 — — 1 5.72
CHEMBL119442 — — 1 5.72
CHEMBL119534 — — 1 5.66
CHEMBL332757 — — 1 5.64
CHEMBL324935 — — 1 5.62
CHEMBL331098 — — 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118387 — IC50 = 45.0 nM 7.35
CHEMBL119793 — IC50 = 56.0 nM 7.25
CHEMBL333201 — IC50 = 95.0 nM 7.02
CHEMBL118271 — IC50 = 140.0 nM 6.85
CHEMBL324251 — IC50 = 290.0 nM 6.54
CHEMBL332685 — IC50 = 380.0 nM 6.42
CHEMBL420880 — IC50 = 390.0 nM 6.41
CHEMBL119806 — IC50 = 410.0 nM 6.39
CHEMBL333135 — IC50 = 630.0 nM 6.20
CHEMBL324488 — IC50 = 720.0 nM 6.14
CHEMBL332450 — IC50 = 760.0 nM 6.12
CHEMBL118609 — IC50 = 890.0 nM 6.05
CHEMBL331173 — IC50 = 980.0 nM 6.01
CHEMBL334082 — IC50 = 1000.0 nM 6.00
CHEMBL118863 — IC50 = 1200.0 nM 5.92
CHEMBL332060 — IC50 = 1200.0 nM 5.92
CHEMBL119638 — IC50 = 1300.0 nM 5.89
CHEMBL420762 MOZAVAPTAN IC50 = 1400.0 nM 5.85
CHEMBL331164 — IC50 = 1400.0 nM 5.85
CHEMBL118922 — IC50 = 1600.0 nM 5.80
CHEMBL333139 — IC50 = 1600.0 nM 5.80
CHEMBL118660 — IC50 = 1600.0 nM 5.80
CHEMBL334009 — IC50 = 1700.0 nM 5.77
CHEMBL333652 — IC50 = 1800.0 nM 5.75
CHEMBL119442 — IC50 = 1910.0 nM 5.72
CHEMBL118878 — IC50 = 1900.0 nM 5.72
CHEMBL119534 — IC50 = 2200.0 nM 5.66
CHEMBL332757 — IC50 = 2300.0 nM 5.64
CHEMBL324935 — IC50 = 2400.0 nM 5.62
CHEMBL331098 — IC50 = 2400.0 nM 5.62
CHEMBL118244 — IC50 = 2500.0 nM 5.60
CHEMBL119318 — IC50 = 2600.0 nM 5.58
CHEMBL333597 — IC50 = 2600.0 nM 5.58
CHEMBL333055 — IC50 = 2700.0 nM 5.57
CHEMBL119671 — IC50 = 2800.0 nM 5.55
CHEMBL120449 — IC50 = 2800.0 nM 5.55
CHEMBL118562 — IC50 = 2800.0 nM 5.55
CHEMBL118270 — IC50 = 3000.0 nM 5.52
CHEMBL334225 — IC50 = 3000.0 nM 5.52
CHEMBL118220 — IC50 = 3100.0 nM 5.51
CHEMBL119730 — IC50 = 3200.0 nM 5.50
CHEMBL119591 — IC50 = 3200.0 nM 5.50
CHEMBL323802 — IC50 = 3200.0 nM 5.50
CHEMBL117566 — IC50 = 3300.0 nM 5.48
CHEMBL118892 — IC50 = 4000.0 nM 5.40
CHEMBL115434 — IC50 = 4300.0 nM 5.37
CHEMBL118829 — IC50 = 5100.0 nM 5.29
CHEMBL119551 — IC50 = 5100.0 nM 5.29
CHEMBL121455 — IC50 = 6400.0 nM 5.19
CHEMBL116820 — IC50 = 7700.0 nM 5.11