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Assay Detail

CHEMBL4477103

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

Binding
Agonist activity at human AT1R expressed in HEK293 cells incubated for 60 mins by luminescence based beta-arrestin recruitment assay
81
Total Activities
81
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

beta-arrestin effectors and compositions and methods of use thereof
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 81 6.65 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL77838 1 8.47
CHEMBL2028943 1 8.10
CHEMBL4544902 1 8.10
CHEMBL312754 1 8.04
CHEMBL4546799 1 8.04
CHEMBL408403 ANGIOTENSIN II 4.0 1 8.01
CHEMBL4483576 1 8.00
CHEMBL938 SARALASIN 4.0 1 7.96
CHEMBL4518530 1 7.92
CHEMBL4514079 1 7.89
CHEMBL4297447 TRV-120027 2.0 1 7.77
CHEMBL4567667 1 7.70
CHEMBL2392353 ANGIOTENSIN-II 1 7.68
CHEMBL4591448 1 7.60
CHEMBL4533618 1 7.60
CHEMBL4560224 1 7.52
CHEMBL4564950 1 7.51
CHEMBL4591857 1 7.50
CHEMBL4549405 1 7.48
CHEMBL4515848 1 7.41
CHEMBL4536886 1 7.40
CHEMBL4577691 1 7.38
CHEMBL4438122 1 7.36
CHEMBL4535997 1 7.30
CHEMBL4564617 1 7.20
CHEMBL4577270 1 7.12
CHEMBL4562270 1 7.10
CHEMBL4593310 1 7.02
CHEMBL4518318 1 7.00
CHEMBL4535678 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL77838 EC50 = 3.4 nM 8.47
CHEMBL2028943 EC50 = 8.0 nM 8.10
CHEMBL4544902 EC50 = 7.9 nM 8.10
CHEMBL312754 EC50 = 9.2 nM 8.04
CHEMBL4546799 EC50 = 9.2 nM 8.04
CHEMBL408403 ANGIOTENSIN II EC50 = 9.7 nM 8.01
CHEMBL4483576 EC50 = 10.0 nM 8.00
CHEMBL938 SARALASIN EC50 = 11.0 nM 7.96
CHEMBL4518530 EC50 = 12.0 nM 7.92
CHEMBL4514079 EC50 = 13.0 nM 7.89
CHEMBL4297447 TRV-120027 EC50 = 17.0 nM 7.77
CHEMBL4567667 EC50 = 20.0 nM 7.70
CHEMBL2392353 ANGIOTENSIN-II EC50 = 21.0 nM 7.68
CHEMBL4533618 EC50 = 25.0 nM 7.60
CHEMBL4591448 EC50 = 25.0 nM 7.60
CHEMBL4560224 EC50 = 30.0 nM 7.52
CHEMBL4564950 EC50 = 31.0 nM 7.51
CHEMBL4591857 EC50 = 32.0 nM 7.50
CHEMBL4549405 EC50 = 33.0 nM 7.48
CHEMBL4515848 EC50 = 39.0 nM 7.41
CHEMBL4536886 EC50 = 40.0 nM 7.40
CHEMBL4577691 EC50 = 42.0 nM 7.38
CHEMBL4438122 EC50 = 44.0 nM 7.36
CHEMBL4535997 EC50 = 50.0 nM 7.30
CHEMBL4564617 EC50 = 63.0 nM 7.20
CHEMBL4577270 EC50 = 75.0 nM 7.12
CHEMBL4562270 EC50 = 79.0 nM 7.10
CHEMBL4593310 EC50 = 95.0 nM 7.02
CHEMBL4518318 EC50 = 100.0 nM 7.00
CHEMBL4535678 EC50 = 100.0 nM 7.00
CHEMBL4573250 EC50 = 160.0 nM 6.80
CHEMBL4518420 EC50 = 160.0 nM 6.80
CHEMBL4542709 EC50 = 200.0 nM 6.70
CHEMBL4555119 EC50 = 210.0 nM 6.68
CHEMBL4588946 EC50 = 220.0 nM 6.66
CHEMBL4577692 EC50 = 250.0 nM 6.60
CHEMBL4547423 EC50 = 270.0 nM 6.57
CHEMBL4522246 EC50 = 320.0 nM 6.50
CHEMBL4529051 EC50 = 330.0 nM 6.48
CHEMBL4516768 EC50 = 330.0 nM 6.48
CHEMBL4579604 EC50 = 340.0 nM 6.47
CHEMBL4515768 EC50 = 390.0 nM 6.41
CHEMBL4557984 EC50 = 400.0 nM 6.40
CHEMBL4543860 EC50 = 430.0 nM 6.37
CHEMBL4517561 EC50 = 450.0 nM 6.35
CHEMBL4545153 EC50 = 480.0 nM 6.32
CHEMBL4551431 EC50 = 530.0 nM 6.28
CHEMBL4588454 EC50 = 550.0 nM 6.26
CHEMBL4545399 EC50 = 590.0 nM 6.23
CHEMBL4590589 EC50 = 630.0 nM 6.20