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Assay Detail

CHEMBL648761

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Binding
Inhibition of [125I]AII binding to Angiotensin II receptor, type 1 of rat mesenteric arteries
ChEMBL ↗
65
Total Activities
64
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Angiotensin II receptor (CHEMBL2094112) ↗
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Potent nonpeptide angiotensin II receptor antagonists. 2. 1-(Carboxybenzyl)imidazole-5-acrylic acids.
Keenan RM, Weinstock J, Finkelstein JA, Franz RG, Gaitanopoulos DE, Girard GR, Hill DT, Morgan TM, Samanen JM, Peishoff CE.
J Med Chem (1993) 36 : 1880 -1892
PubMed 8515425 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 65 7.33 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL292892 — — 1 9.82
CHEMBL294686 — — 1 9.52
CHEMBL293091 — — 1 9.40
CHEMBL56211 — — 1 9.25
CHEMBL55510 — — 1 9.23
CHEMBL294415 — — 1 9.10
CHEMBL813 EPROSARTAN 4.0 2 9.00
CHEMBL57309 — — 1 9.00
CHEMBL37679 — — 1 8.84
CHEMBL54421 — — 1 8.60
CHEMBL56333 — — 1 8.49
CHEMBL56497 — — 1 8.48
CHEMBL291955 — — 1 8.37
CHEMBL56160 — — 1 8.35
CHEMBL299064 — — 1 8.34
CHEMBL299954 — — 1 8.32
CHEMBL56522 — — 1 8.30
CHEMBL56690 — — 1 8.18
CHEMBL54645 — — 1 7.82
CHEMBL40089 — — 1 7.68
CHEMBL300566 — — 1 7.68
CHEMBL54711 — — 1 7.66
CHEMBL57620 — — 1 7.63
CHEMBL55950 — — 1 7.56
CHEMBL291086 — — 1 7.51
CHEMBL59580 — — 1 7.47
CHEMBL287936 — — 1 7.47
CHEMBL291688 — — 1 7.47
CHEMBL56574 — — 1 7.46
CHEMBL293706 — — 1 7.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL292892 — IC50 = 0.15 nM 9.82
CHEMBL294686 — IC50 = 0.3 nM 9.52
CHEMBL293091 — IC50 = 0.4 nM 9.40
CHEMBL56211 — IC50 = 0.56 nM 9.25
CHEMBL55510 — IC50 = 0.59 nM 9.23
CHEMBL294415 — IC50 = 0.8 nM 9.10
CHEMBL813 EPROSARTAN IC50 = 1.0 nM 9.00
CHEMBL57309 — IC50 = 1.0 nM 9.00
CHEMBL37679 — IC50 = 1.45 nM 8.84
CHEMBL54421 — IC50 = 2.5 nM 8.60
CHEMBL56333 — IC50 = 3.25 nM 8.49
CHEMBL56497 — IC50 = 3.3 nM 8.48
CHEMBL291955 — IC50 = 4.26 nM 8.37
CHEMBL56160 — IC50 = 4.5 nM 8.35
CHEMBL299064 — IC50 = 4.6 nM 8.34
CHEMBL299954 — IC50 = 4.81 nM 8.32
CHEMBL56522 — IC50 = 5.0 nM 8.30
CHEMBL56690 — IC50 = 6.6 nM 8.18
CHEMBL54645 — IC50 = 15.0 nM 7.82
CHEMBL40089 — IC50 = 21.0 nM 7.68
CHEMBL300566 — IC50 = 21.0 nM 7.68
CHEMBL54711 — IC50 = 22.0 nM 7.66
CHEMBL57620 — IC50 = 23.2 nM 7.63
CHEMBL55950 — IC50 = 27.6 nM 7.56
CHEMBL291086 — IC50 = 31.0 nM 7.51
CHEMBL59580 — IC50 = 33.6 nM 7.47
CHEMBL291688 — IC50 = 33.8 nM 7.47
CHEMBL287936 — IC50 = 34.0 nM 7.47
CHEMBL56574 — IC50 = 35.0 nM 7.46
CHEMBL293706 — IC50 = 39.0 nM 7.41
CHEMBL55216 — IC50 = 43.0 nM 7.37
CHEMBL417752 — IC50 = 46.0 nM 7.34
CHEMBL301632 — IC50 = 53.0 nM 7.28
CHEMBL56085 — IC50 = 60.0 nM 7.22
CHEMBL55357 — IC50 = 63.0 nM 7.20
CHEMBL54982 — IC50 = 66.0 nM 7.18
CHEMBL54446 — IC50 = 94.2 nM 7.03
CHEMBL54576 — IC50 = 118.0 nM 6.93
CHEMBL54459 — IC50 = 123.0 nM 6.91
CHEMBL57677 — IC50 = 127.0 nM 6.90
CHEMBL59157 — IC50 = 130.0 nM 6.89
CHEMBL291329 — IC50 = 163.0 nM 6.79
CHEMBL292165 — IC50 = 180.0 nM 6.75
CHEMBL58981 — IC50 = 210.0 nM 6.68
CHEMBL54696 — IC50 = 230.0 nM 6.64
CHEMBL59094 — IC50 = 248.0 nM 6.61
CHEMBL55231 — IC50 = 250.0 nM 6.60
CHEMBL293495 — IC50 = 260.0 nM 6.58
CHEMBL293940 — IC50 = 310.0 nM 6.51
CHEMBL813 EPROSARTAN IC50 = 363.0 nM 6.44