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Assay Detail

CHEMBL649532

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

Functional
Antagonistic activity against Angiotensin II receptor type 1 in rat uterus
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Uterus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Angiotensin II receptor (AT-1) type-1 (CHEMBL2094250)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Structural comparison between type I and type II antagonists: possible implications in the drug design of AT1 antagonists.
Roumelioti P, Tselios T, Alexopoulos K, Mavromoustakos T, Kolocouris A, Moore GJ, Matsoukas JM.
Bioorg Med Chem Lett (2000) 10 : 755 -758
PubMed 10782679 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 6.83 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL404594 1 8.10
CHEMBL350715 1 7.80
CHEMBL2371021 1 7.50
CHEMBL216533 1 6.70
CHEMBL2371453 1 6.60
CHEMBL166204 1 5.70
CHEMBL264335 1 5.40
CHEMBL349256 1 -
CHEMBL350132 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL404594 Kd = 7.943 nM 8.10
CHEMBL350715 Kd = 15.85 nM 7.80
CHEMBL2371021 Kd = 31.62 nM 7.50
CHEMBL216533 Kd = 199.53 nM 6.70
CHEMBL2371453 Kd = 251.19 nM 6.60
CHEMBL166204 Kd = 1995.26 nM 5.70
CHEMBL264335 Kd = 3981.07 nM 5.40
CHEMBL349256 Kd > 15848.93 nM -
CHEMBL350132 Kd > 15848.93 nM -