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Assay Detail

CHEMBL3736606

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

Binding
Displacement of [125I]Sar1Ile8-Ang2 from human AT1 receptor expressed in CHO-K1 cell membranes after 180 mins
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of novel, potent and low-toxicity angiotensin II receptor type 1 (AT1) blockers: Design, synthesis and biological evaluation of 6-substituted aminocarbonyl benzimidazoles with a chiral center.
Han XF, He X, Wang M, Xu D, Hao LP, Liang AH, Zhang J, Zhou ZM.
Eur J Med Chem (2015) 103 : 473 -487
PubMed 26397395 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 7.03 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3735744 1 8.96
CHEMBL3736514 1 8.85
CHEMBL3736244 1 8.57
CHEMBL3735290 1 8.46
CHEMBL3735409 1 8.30
CHEMBL3734891 1 8.20
CHEMBL3736440 1 8.14
CHEMBL2058860 1 7.78
CHEMBL3736295 1 7.71
CHEMBL3735588 1 7.64
CHEMBL2435818 1 7.64
CHEMBL191 LOSARTAN 4.0 1 7.54
CHEMBL3735769 1 7.41
CHEMBL3735652 1 7.39
CHEMBL3736451 1 7.24
CHEMBL3736319 1 7.24
CHEMBL3735804 1 7.21
CHEMBL3735098 1 7.16
CHEMBL3734763 1 7.06
CHEMBL3736257 1 7.04
CHEMBL3734819 1 7.03
CHEMBL3735333 1 6.98
CHEMBL3735487 1 6.97
CHEMBL3734949 1 6.89
CHEMBL3735446 1 6.80
CHEMBL3735641 1 6.79
CHEMBL3735492 1 6.67
CHEMBL3735839 1 6.53
CHEMBL3734989 1 6.46
CHEMBL3736166 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3735744 IC50 = 1.1 nM 8.96
CHEMBL3736514 IC50 = 1.4 nM 8.85
CHEMBL3736244 IC50 = 2.7 nM 8.57
CHEMBL3735290 IC50 = 3.5 nM 8.46
CHEMBL3735409 IC50 = 5.0 nM 8.30
CHEMBL3734891 IC50 = 6.3 nM 8.20
CHEMBL3736440 IC50 = 7.3 nM 8.14
CHEMBL2058860 IC50 = 16.7 nM 7.78
CHEMBL3736295 IC50 = 19.5 nM 7.71
CHEMBL3735588 IC50 = 23.0 nM 7.64
CHEMBL2435818 IC50 = 23.1 nM 7.64
CHEMBL191 LOSARTAN IC50 = 28.6 nM 7.54
CHEMBL3735769 IC50 = 38.9 nM 7.41
CHEMBL3735652 IC50 = 40.4 nM 7.39
CHEMBL3736319 IC50 = 57.9 nM 7.24
CHEMBL3736451 IC50 = 57.4 nM 7.24
CHEMBL3735804 IC50 = 61.2 nM 7.21
CHEMBL3735098 IC50 = 70.0 nM 7.16
CHEMBL3734763 IC50 = 87.2 nM 7.06
CHEMBL3736257 IC50 = 90.5 nM 7.04
CHEMBL3734819 IC50 = 93.9 nM 7.03
CHEMBL3735333 IC50 = 104.0 nM 6.98
CHEMBL3735487 IC50 = 106.5 nM 6.97
CHEMBL3734949 IC50 = 128.6 nM 6.89
CHEMBL3735446 IC50 = 156.8 nM 6.80
CHEMBL3735641 IC50 = 161.1 nM 6.79
CHEMBL3735492 IC50 = 214.4 nM 6.67
CHEMBL3735839 IC50 = 293.1 nM 6.53
CHEMBL3734989 IC50 = 342.8 nM 6.46
CHEMBL3736166 IC50 = 366.3 nM 6.44
CHEMBL3736202 IC50 = 486.8 nM 6.31
CHEMBL3735558 IC50 = 503.3 nM 6.30
CHEMBL3736336 IC50 = 495.8 nM 6.30
CHEMBL3735227 IC50 = 621.6 nM 6.21
CHEMBL3735653 IC50 = 609.2 nM 6.21
CHEMBL3735940 IC50 = 671.4 nM 6.17
CHEMBL3736346 IC50 = 699.3 nM 6.16
CHEMBL3735831 IC50 = 738.4 nM 6.13
CHEMBL3735390 IC50 = 788.4 nM 6.10
CHEMBL3734859 IC50 = 1117.3 nM 5.95
CHEMBL3736338 IC50 = 1368.1 nM 5.86
CHEMBL3734815 IC50 = 1536.6 nM 5.81
CHEMBL3735910 IC50 = 1534.5 nM 5.81