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Assay Detail

CHEMBL652870

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Binding
Tested for in vitro binding affinity against angiotensin I (AT1) receptor to competitively block the specific binding of [125I]- [Sar1,Ile8] AII to a rabbit aorta AT1 receptor preparation
ChEMBL ↗
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Type-1 angiotensin II receptor (CHEMBL3948) ↗
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Triazolinone biphenylsulfonamides as angiotensin II receptor antagonists with high affinity for both the AT1 and AT2 subtypes.
Chang LL, Ashton WT, Flanagan KL, Chen TB, O'Malley SS, Zingaro GJ, Siegl PK, Kivlighn SD, Lotti VJ, Chang RS.
J Med Chem (1994) 37 : 4464 -4478
PubMed 7799397 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 9.39 10.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL138690 — — 1 10.37
CHEMBL265797 — — 1 10.28
CHEMBL341828 — — 1 10.14
CHEMBL343309 — — 1 10.10
CHEMBL316300 — — 1 9.96
CHEMBL341934 — — 1 9.96
CHEMBL343142 — — 1 9.96
CHEMBL140708 — — 1 9.92
CHEMBL338101 — — 1 9.85
CHEMBL139452 — — 1 9.85
CHEMBL136465 — — 1 9.80
CHEMBL96075 — — 1 9.80
CHEMBL93907 — — 1 9.77
CHEMBL337118 — — 1 9.74
CHEMBL334300 — — 1 9.68
CHEMBL275552 — — 1 9.68
CHEMBL435792 — — 1 9.68
CHEMBL344597 — — 1 9.60
CHEMBL341783 — — 1 9.60
CHEMBL139041 — — 1 9.59
CHEMBL276674 — — 1 9.54
CHEMBL343634 — — 1 9.52
CHEMBL342492 — — 1 9.43
CHEMBL141592 — — 1 9.39
CHEMBL139325 — — 1 9.39
CHEMBL342605 — — 1 9.38
CHEMBL279629 L-159913 — 1 9.37
CHEMBL292150 — — 1 9.35
CHEMBL342843 — — 1 9.25
CHEMBL344387 — — 1 9.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL138690 — IC50 = 0.043 nM 10.37
CHEMBL265797 — IC50 = 0.052 nM 10.28
CHEMBL341828 — IC50 = 0.072 nM 10.14
CHEMBL343309 — IC50 = 0.08 nM 10.10
CHEMBL316300 — IC50 = 0.11 nM 9.96
CHEMBL341934 — IC50 = 0.11 nM 9.96
CHEMBL343142 — IC50 = 0.11 nM 9.96
CHEMBL140708 — IC50 = 0.12 nM 9.92
CHEMBL338101 — IC50 = 0.14 nM 9.85
CHEMBL139452 — IC50 = 0.14 nM 9.85
CHEMBL136465 — IC50 = 0.16 nM 9.80
CHEMBL96075 — IC50 = 0.16 nM 9.80
CHEMBL93907 — IC50 = 0.17 nM 9.77
CHEMBL337118 — IC50 = 0.18 nM 9.74
CHEMBL435792 — IC50 = 0.21 nM 9.68
CHEMBL334300 — IC50 = 0.21 nM 9.68
CHEMBL275552 — IC50 = 0.21 nM 9.68
CHEMBL344597 — IC50 = 0.25 nM 9.60
CHEMBL341783 — IC50 = 0.25 nM 9.60
CHEMBL139041 — IC50 = 0.26 nM 9.59
CHEMBL276674 — IC50 = 0.29 nM 9.54
CHEMBL343634 — IC50 = 0.3 nM 9.52
CHEMBL342492 — IC50 = 0.37 nM 9.43
CHEMBL141592 — IC50 = 0.41 nM 9.39
CHEMBL139325 — IC50 = 0.41 nM 9.39
CHEMBL342605 — IC50 = 0.42 nM 9.38
CHEMBL279629 L-159913 IC50 = 0.43 nM 9.37
CHEMBL292150 — IC50 = 0.45 nM 9.35
CHEMBL342843 — IC50 = 0.56 nM 9.25
CHEMBL344387 — IC50 = 0.56 nM 9.25
CHEMBL344811 — IC50 = 0.63 nM 9.20
CHEMBL19018 — IC50 = 0.78 nM 9.11
CHEMBL344467 — IC50 = 0.85 nM 9.07
CHEMBL140619 — IC50 = 0.9 nM 9.05
CHEMBL139582 — IC50 = 1.0 nM 9.00
CHEMBL337588 — IC50 = 1.4 nM 8.85
CHEMBL341715 — IC50 = 1.6 nM 8.80
CHEMBL302102 — IC50 = 1.7 nM 8.77
CHEMBL138654 — IC50 = 1.8 nM 8.74
CHEMBL344466 — IC50 = 2.4 nM 8.62
CHEMBL343719 — IC50 = 5.8 nM 8.24
CHEMBL341986 — IC50 = 24.0 nM 7.62
CHEMBL293501 — IC50 = 31.0 nM 7.51