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Assay Detail

CHEMBL5442690

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

Functional
GPCR PRESTO-Tango dose-response in antagonist mode with target: AGTR1
15
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HTLA
Category GPCR beta-arrestin recruitment assay
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Type-1 angiotensin II receptor (CHEMBL227)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

EUbOPEN Chemogenomics Library - GPCR Dose-Respose
EUbOPEN
(2024)
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.59 9.22
EC50 1 5.90 5.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2440454 1 9.22
CHEMBL1513 IRBESARTAN 4.0 1 8.52
CHEMBL1017 TELMISARTAN 4.0 1 8.27
CHEMBL130896 1 7.78
CHEMBL191 LOSARTAN 4.0 1 7.60
CHEMBL484929 1 5.90
CHEMBL1256876 1 5.50
CHEMBL1766103 1 5.44
CHEMBL329650 1 5.43
CHEMBL1474387 1 5.38
CHEMBL531742 1 5.36
CHEMBL103769 1 5.32
CHEMBL4743495 1 5.20
CHEMBL238804 SELEXIPAG 4.0 1 -
CHEMBL1200517 DIHYDROERGOTAMINE MESYLATE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2440454 IC50 = 0.6063 nM 9.22
CHEMBL1513 IRBESARTAN IC50 = 2.999 nM 8.52
CHEMBL1017 TELMISARTAN IC50 = 5.398 nM 8.27
CHEMBL130896 IC50 = 16.59 nM 7.78
CHEMBL191 LOSARTAN IC50 = 24.86 nM 7.60
CHEMBL484929 EC50 = 1259.37 nM 5.90
CHEMBL1256876 IC50 = 3130.24 nM 5.50
CHEMBL1766103 IC50 = 3604.72 nM 5.44
CHEMBL329650 IC50 = 3697.15 nM 5.43
CHEMBL1474387 IC50 = 4186.31 nM 5.38
CHEMBL531742 IC50 = 4409.59 nM 5.36
CHEMBL103769 IC50 = 4824.87 nM 5.32
CHEMBL4743495 IC50 = 6257.99 nM 5.20
CHEMBL238804 SELEXIPAG IC50 > 10000.0 nM -
CHEMBL1200517 DIHYDROERGOTAMINE MESYLATE IC50 > 10000.0 nM -