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Assay Detail

CHEMBL652266

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Functional
In vitro antagonist activity against Angiotensin II receptor was measured in the rabbit aorta strip assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Angiotensin II receptor (CHEMBL2094256)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

The importance of residues 2 (arginine) and 6 (histidine) in high-affinity angiotensin II antagonists.
Samanen J, Brandeis E, Narindray D, Adams W, Cash T, Yellin T, Regoli D.
J Med Chem (1988) 31 : 737 -741
PubMed 3351849 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 28 7.48 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL404594 1 9.10
CHEMBL2371400 1 8.79
CHEMBL2371388 1 8.78
CHEMBL2371393 1 8.25
CHEMBL2371409 1 7.75
CHEMBL2371401 1 7.75
CHEMBL2371399 1 7.50
CHEMBL2371394 1 7.50
CHEMBL2371411 1 7.50
CHEMBL2371425 1 7.40
CHEMBL2371429 1 7.10
CHEMBL2371392 1 7.00
CHEMBL2371391 1 7.00
CHEMBL2371396 1 6.75
CHEMBL2371415 1 6.75
CHEMBL2371406 1 6.20
CHEMBL2371417 1 6.00
CHEMBL2371424 1 -
CHEMBL2371434 1 -
CHEMBL2371435 1 -
CHEMBL2371403 1 -
CHEMBL2371433 1 -
CHEMBL2371413 1 -
CHEMBL2371423 1 -
CHEMBL2371384 1 -
CHEMBL2371426 1 -
CHEMBL1702539 1 -
CHEMBL2112029 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL404594 Kd = 0.7943 nM 9.10
CHEMBL2371400 Kd = 1.622 nM 8.79
CHEMBL2371388 Kd = 1.66 nM 8.78
CHEMBL2371393 Kd = 5.623 nM 8.25
CHEMBL2371409 Kd = 17.78 nM 7.75
CHEMBL2371401 Kd = 17.78 nM 7.75
CHEMBL2371399 Kd = 31.62 nM 7.50
CHEMBL2371394 Kd = 31.62 nM 7.50
CHEMBL2371411 Kd = 31.62 nM 7.50
CHEMBL2371425 Kd = 39.81 nM 7.40
CHEMBL2371429 Kd = 79.43 nM 7.10
CHEMBL2371392 Kd = 100.0 nM 7.00
CHEMBL2371391 Kd = 100.0 nM 7.00
CHEMBL2371396 Kd = 177.83 nM 6.75
CHEMBL2371415 Kd = 177.83 nM 6.75
CHEMBL2371406 Kd = 630.96 nM 6.20
CHEMBL2371417 Kd = 1000.0 nM 6.00
CHEMBL2371424 Kd > 1000.0 nM -
CHEMBL2371434 Kd > 1000.0 nM -
CHEMBL2371435 Kd > 1000.0 nM -
CHEMBL2371403 Kd = 1000000000.0 nM -
CHEMBL2371433 Kd > 1000.0 nM -
CHEMBL2371413 Kd > 1000.0 nM -
CHEMBL2371423 Kd > 1000.0 nM -
CHEMBL2371384 Kd = 1000000000.0 nM -
CHEMBL2371426 Kd = 1000000000.0 nM -
CHEMBL1702539 Kd > 1000.0 nM -
CHEMBL2112029 Kd << 6.0 nM -