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Assay Detail

CHEMBL770465

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

Functional
In vitro antagonist activity (ANG II like) expressed as percent activity relative to ANG II in rabbit aorta strip assay.
25
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Aorta
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Angiotensin II receptor (CHEMBL2094112)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

An investigation of angiotensin II agonist and antagonist analogues with 5,5-dimethylthiazolidine-4-carboxylic acid and other constrained amino acids.
Samanen J, Cash T, Narindray D, Brandeis E, Adams W, Weideman H, Yellin T, Regoli D.
J Med Chem (1991) 34 : 3036 -3043
PubMed 1920354 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 25 8.31 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2370349 1 9.70
CHEMBL328167 1 9.60
CHEMBL404594 1 9.10
CHEMBL2370367 1 9.00
CHEMBL2364552 1 9.00
CHEMBL2370346 1 9.00
CHEMBL321952 1 8.90
CHEMBL317439 1 8.70
CHEMBL408595 1 8.70
CHEMBL312754 2 8.61
CHEMBL322627 1 8.40
CHEMBL263278 1 8.30
CHEMBL317253 1 8.30
CHEMBL263360 1 8.25
CHEMBL318091 1 8.00
CHEMBL385919 1 7.64
CHEMBL2370356 1 7.50
CHEMBL2311163 1 7.50
CHEMBL103336 1 7.50
CHEMBL406385 1 7.17
CHEMBL427769 1 7.00
CHEMBL2370348 1 6.70
CHEMBL267751 1 -
CHEMBL2370371 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2370349 Kd = 0.1995 nM 9.70
CHEMBL328167 Kd = 0.2512 nM 9.60
CHEMBL404594 Kd = 0.7943 nM 9.10
CHEMBL2370367 Kd = 1.0 nM 9.00
CHEMBL2364552 Kd = 1.0 nM 9.00
CHEMBL2370346 Kd = 1.0 nM 9.00
CHEMBL321952 Kd = 1.259 nM 8.90
CHEMBL317439 Kd = 1.995 nM 8.70
CHEMBL408595 Kd = 1.995 nM 8.70
CHEMBL312754 Kd = 2.455 nM 8.61
CHEMBL312754 Kd = 2.512 nM 8.60
CHEMBL322627 Kd = 3.981 nM 8.40
CHEMBL317253 Kd = 5.012 nM 8.30
CHEMBL263278 Kd = 5.012 nM 8.30
CHEMBL263360 Kd = 5.623 nM 8.25
CHEMBL318091 Kd = 10.0 nM 8.00
CHEMBL385919 Kd = 22.91 nM 7.64
CHEMBL2370356 Kd = 31.62 nM 7.50
CHEMBL2311163 Kd = 31.62 nM 7.50
CHEMBL103336 Kd = 31.62 nM 7.50
CHEMBL406385 Kd = 67.61 nM 7.17
CHEMBL427769 Kd = 100.0 nM 7.00
CHEMBL2370348 Kd = 199.53 nM 6.70
CHEMBL267751 Kd > 1000.0 nM -
CHEMBL2370371 Kd > 1000.0 nM -