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Assay Detail

CHEMBL648763

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Binding
Inhibitory concentration was evaluated by measuring displacement of [3H]AII from rat liver Angiotensin II receptor, type 1
ChEMBL ↗
46
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Angiotensin II receptor (AT-1) type-1 (CHEMBL2094250) ↗
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Diphenylpropionic acids as new AT1 selective angiotensin II antagonists.
Almansa C, Gómez LA, Cavalcanti FL, de Arriba AF, Rodríguez R, Carceller E, García-Rafanell J, Forn J.
J Med Chem (1996) 39 : 2197 -2206
PubMed 8667363 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 6.61 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL308286 — — 2 7.36
CHEMBL308659 — — 1 7.30
CHEMBL71048 — — 1 7.24
CHEMBL191 LOSARTAN 4.0 1 7.23
CHEMBL71485 — — 3 7.16
CHEMBL307272 — — 1 7.15
CHEMBL309166 — — 1 7.11
CHEMBL69647 — — 1 7.08
CHEMBL74004 — — 2 7.04
CHEMBL71632 — — 1 7.03
CHEMBL69028 — — 1 6.96
CHEMBL302136 — — 1 6.92
CHEMBL68510 — — 1 6.92
CHEMBL307963 — — 2 6.92
CHEMBL71767 — — 1 6.89
CHEMBL302794 — — 1 6.80
CHEMBL71875 — — 1 6.77
CHEMBL69246 — — 3 6.75
CHEMBL304614 — — 1 6.70
CHEMBL432145 — — 1 6.70
CHEMBL303885 — — 1 6.68
CHEMBL304289 — — 1 6.62
CHEMBL70642 — — 1 6.60
CHEMBL306013 — — 1 6.50
CHEMBL303430 — — 1 6.48
CHEMBL308985 — — 1 6.44
CHEMBL70252 — — 1 6.37
CHEMBL309108 — — 1 6.35
CHEMBL304795 — — 1 6.35
CHEMBL449655 — — 1 6.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL308286 — IC50 = 44.0 nM 7.36
CHEMBL308659 — IC50 = 50.0 nM 7.30
CHEMBL71048 — IC50 = 58.0 nM 7.24
CHEMBL191 LOSARTAN IC50 = 59.0 nM 7.23
CHEMBL71485 — IC50 = 69.0 nM 7.16
CHEMBL71485 — IC50 = 71.0 nM 7.15
CHEMBL307272 — IC50 = 71.0 nM 7.15
CHEMBL71485 — IC50 = 76.0 nM 7.12
CHEMBL309166 — IC50 = 78.0 nM 7.11
CHEMBL69647 — IC50 = 83.0 nM 7.08
CHEMBL74004 — IC50 = 92.0 nM 7.04
CHEMBL71632 — IC50 = 94.0 nM 7.03
CHEMBL69028 — IC50 = 110.0 nM 6.96
CHEMBL302136 — IC50 = 120.0 nM 6.92
CHEMBL307963 — IC50 = 120.0 nM 6.92
CHEMBL68510 — IC50 = 120.0 nM 6.92
CHEMBL74004 — IC50 = 130.0 nM 6.89
CHEMBL71767 — IC50 = 130.0 nM 6.89
CHEMBL302794 — IC50 = 160.0 nM 6.80
CHEMBL307963 — IC50 = 170.0 nM 6.77
CHEMBL71875 — IC50 = 170.0 nM 6.77
CHEMBL69246 — IC50 = 180.0 nM 6.75
CHEMBL304614 — IC50 = 200.0 nM 6.70
CHEMBL432145 — IC50 = 200.0 nM 6.70
CHEMBL303885 — IC50 = 210.0 nM 6.68
CHEMBL304289 — IC50 = 240.0 nM 6.62
CHEMBL69246 — IC50 = 250.0 nM 6.60
CHEMBL70642 — IC50 = 250.0 nM 6.60
CHEMBL308286 — IC50 = 290.0 nM 6.54
CHEMBL306013 — IC50 = 320.0 nM 6.50
CHEMBL303430 — IC50 = 330.0 nM 6.48
CHEMBL308985 — IC50 = 360.0 nM 6.44
CHEMBL70252 — IC50 = 430.0 nM 6.37
CHEMBL69246 — IC50 = 440.0 nM 6.36
CHEMBL309108 — IC50 = 450.0 nM 6.35
CHEMBL304795 — IC50 = 450.0 nM 6.35
CHEMBL449655 — IC50 = 590.0 nM 6.23
CHEMBL431970 — IC50 = 600.0 nM 6.22
CHEMBL67861 — IC50 = 1100.0 nM 5.96
CHEMBL70712 — IC50 = 3700.0 nM 5.43
CHEMBL305189 — IC50 = 4800.0 nM 5.32
CHEMBL308916 — IC50 = 5300.0 nM 5.28
CHEMBL71902 — IC50 = 5600.0 nM 5.25
CHEMBL304607 — IC50 = 8300.0 nM 5.08
CHEMBL307862 — IC50 > 10000.0 nM -
CHEMBL68947 — IC50 > 10000.0 nM -