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Assay Detail

CHEMBL643135

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

Functional
Inhibitory activity as antagonist of AII on guinea pig ileum
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

Synthesis and biological activity of angiotensin II analogues containing a Val-His replacement, Val psi[CH(CONH2)NH]His.
Mohan R, Chou YL, Bihovsky R, Lumma WC, Erhardt PW, Shaw KJ.
J Med Chem (1991) 34 : 2402 -2410
PubMed 1875337 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.79 10.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL938 SARALASIN 4.0 1 10.18
CHEMBL404594 1 9.68
CHEMBL77838 1 9.35
CHEMBL312754 1 8.24
CHEMBL2369863 1 6.48
CHEMBL309651 1 -
CHEMBL418901 1 -
CHEMBL76890 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL938 SARALASIN IC50 = 0.066 nM 10.18
CHEMBL404594 IC50 = 0.21 nM 9.68
CHEMBL77838 IC50 = 0.45 nM 9.35
CHEMBL312754 IC50 = 5.8 nM 8.24
CHEMBL2369863 IC50 = 330.0 nM 6.48
CHEMBL309651 IC50 > 15000.0 nM -
CHEMBL418901 IC50 > 15000.0 nM -
CHEMBL76890 IC50 > 15000.0 nM -