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Assay Detail

CHEMBL651250

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Binding
In vitro inhibitory activity against angiotensin II rat midbrain AT2 receptor using radioligand [125I]-Sar Ile-AII
ChEMBL ↗
101
Total Activities
101
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Type-2 angiotensin II receptor (CHEMBL257) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Triazolinone biphenylsulfonamide derivatives as orally active angiotensin II antagonists with potent AT1 receptor affinity and enhanced AT2 affinity.
Ashton WT, Chang LL, Flanagan KL, Hutchins SM, Naylor EM, Chakravarty PK, Patchett AA, Greenlee WJ, Chen TB, Faust KA.
J Med Chem (1994) 37 : 2808 -2824
PubMed 8064808 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 101 6.56 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL292150 — — 1 7.77
CHEMBL329290 — — 1 7.60
CHEMBL329942 — — 1 7.58
CHEMBL97446 — — 1 7.52
CHEMBL97394 — — 1 7.46
CHEMBL262296 — — 1 7.46
CHEMBL316300 — — 1 7.44
CHEMBL321363 — — 1 7.37
CHEMBL97020 — — 1 7.35
CHEMBL328941 — — 1 7.34
CHEMBL432822 — — 1 7.34
CHEMBL330533 — — 1 7.28
CHEMBL329693 — — 1 7.26
CHEMBL97075 — — 1 7.22
CHEMBL316904 — — 1 7.14
CHEMBL327563 — — 1 7.12
CHEMBL431619 — — 1 7.12
CHEMBL94145 — — 1 7.10
CHEMBL97688 — — 1 7.10
CHEMBL316273 — — 1 7.09
CHEMBL98453 — — 1 7.08
CHEMBL321367 — — 1 7.07
CHEMBL97271 — — 1 7.06
CHEMBL93606 — — 1 7.00
CHEMBL98426 — — 1 7.00
CHEMBL330464 — — 1 7.00
CHEMBL98126 — — 1 6.96
CHEMBL330165 — — 1 6.96
CHEMBL95198 — — 1 6.96
CHEMBL316655 — — 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL292150 — IC50 = 17.0 nM 7.77
CHEMBL329290 — IC50 = 25.0 nM 7.60
CHEMBL329942 — IC50 = 26.0 nM 7.58
CHEMBL97446 — IC50 = 30.0 nM 7.52
CHEMBL97394 — IC50 = 35.0 nM 7.46
CHEMBL262296 — IC50 = 35.0 nM 7.46
CHEMBL316300 — IC50 = 36.0 nM 7.44
CHEMBL321363 — IC50 = 43.0 nM 7.37
CHEMBL97020 — IC50 = 45.0 nM 7.35
CHEMBL328941 — IC50 = 46.0 nM 7.34
CHEMBL432822 — IC50 = 46.0 nM 7.34
CHEMBL330533 — IC50 = 53.0 nM 7.28
CHEMBL329693 — IC50 = 55.0 nM 7.26
CHEMBL97075 — IC50 = 60.0 nM 7.22
CHEMBL316904 — IC50 = 72.0 nM 7.14
CHEMBL327563 — IC50 = 76.0 nM 7.12
CHEMBL431619 — IC50 = 75.0 nM 7.12
CHEMBL94145 — IC50 = 80.0 nM 7.10
CHEMBL97688 — IC50 = 80.0 nM 7.10
CHEMBL316273 — IC50 = 82.0 nM 7.09
CHEMBL98453 — IC50 = 84.0 nM 7.08
CHEMBL321367 — IC50 = 86.0 nM 7.07
CHEMBL97271 — IC50 = 87.0 nM 7.06
CHEMBL330464 — IC50 = 100.0 nM 7.00
CHEMBL93606 — IC50 = 100.0 nM 7.00
CHEMBL98426 — IC50 = 100.0 nM 7.00
CHEMBL98126 — IC50 = 110.0 nM 6.96
CHEMBL330165 — IC50 = 110.0 nM 6.96
CHEMBL95198 — IC50 = 110.0 nM 6.96
CHEMBL316655 — IC50 = 120.0 nM 6.92
CHEMBL328434 — IC50 = 120.0 nM 6.92
CHEMBL95579 — IC50 = 120.0 nM 6.92
CHEMBL327988 — IC50 = 130.0 nM 6.89
CHEMBL432392 — IC50 = 130.0 nM 6.89
CHEMBL98140 — IC50 = 130.0 nM 6.89
CHEMBL97615 — IC50 = 150.0 nM 6.82
CHEMBL94910 — IC50 = 150.0 nM 6.82
CHEMBL329089 — IC50 = 150.0 nM 6.82
CHEMBL97897 — IC50 = 160.0 nM 6.80
CHEMBL94905 — IC50 = 160.0 nM 6.80
CHEMBL98068 — IC50 = 160.0 nM 6.80
CHEMBL327191 — IC50 = 170.0 nM 6.77
CHEMBL97068 — IC50 = 170.0 nM 6.77
CHEMBL319404 — IC50 = 180.0 nM 6.75
CHEMBL327791 — IC50 = 190.0 nM 6.72
CHEMBL316482 — IC50 = 190.0 nM 6.72
CHEMBL97464 — IC50 = 190.0 nM 6.72
CHEMBL265012 — IC50 = 190.0 nM 6.72
CHEMBL407919 — IC50 = 220.0 nM 6.66
CHEMBL317547 — IC50 = 220.0 nM 6.66