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Assay Detail

CHEMBL645254

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

Binding
pA2 value determined in vitro against angiotensin II receptor, type 1 using rabbit aortic rings
40
Total Activities
40
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

Synthesis and In Vitro evaluation of fused ring heterocyle-containing angiotensin II antagonists.
Zydowsky TM, Winn M, De B, Condon SL, Altenbach RJ, Basha FZ, Boyd SA, Buckner SA, Hancock AA, Lee JY, Mantei RA, Novosad EI, Sorensen BK, Tasker AS, Shiosaki K, Kerkman DJ, Opgenorth TJ, DeBernardis JF
Bioorg Med Chem Lett (1994) 4 : 173 -176
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 40 7.72 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL416477 1 10.30
CHEMBL49410 1 9.93
CHEMBL49663 1 8.59
CHEMBL299741 1 8.58
CHEMBL48270 1 8.53
CHEMBL191 LOSARTAN 4.0 1 8.43
CHEMBL49528 1 8.29
CHEMBL48799 1 8.19
CHEMBL46391 1 8.17
CHEMBL46433 1 8.14
CHEMBL52036 1 8.11
CHEMBL300194 1 8.08
CHEMBL50174 1 8.07
CHEMBL295498 1 8.03
CHEMBL49715 1 8.02
CHEMBL301819 1 7.97
CHEMBL46392 1 7.92
CHEMBL300438 1 7.53
CHEMBL50109 1 7.52
CHEMBL448727 1 7.45
CHEMBL51987 1 7.38
CHEMBL49952 1 7.32
CHEMBL49573 1 7.32
CHEMBL295935 1 7.14
CHEMBL50007 1 7.13
CHEMBL417910 1 7.06
CHEMBL422050 1 7.01
CHEMBL48868 1 6.97
CHEMBL48145 1 6.94
CHEMBL49587 1 6.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL416477 Kd = 0.05012 nM 10.30
CHEMBL49410 Kd = 0.1175 nM 9.93
CHEMBL49663 Kd = 2.57 nM 8.59
CHEMBL299741 Kd = 2.63 nM 8.58
CHEMBL48270 Kd = 2.951 nM 8.53
CHEMBL191 LOSARTAN Kd = 3.715 nM 8.43
CHEMBL49528 Kd = 5.129 nM 8.29
CHEMBL48799 Kd = 6.457 nM 8.19
CHEMBL46391 Kd = 6.761 nM 8.17
CHEMBL46433 Kd = 7.244 nM 8.14
CHEMBL52036 Kd = 7.762 nM 8.11
CHEMBL300194 Kd = 8.318 nM 8.08
CHEMBL50174 Kd = 8.511 nM 8.07
CHEMBL295498 Kd = 9.333 nM 8.03
CHEMBL49715 Kd = 9.55 nM 8.02
CHEMBL301819 Kd = 10.72 nM 7.97
CHEMBL46392 Kd = 12.02 nM 7.92
CHEMBL300438 Kd = 29.51 nM 7.53
CHEMBL50109 Kd = 30.2 nM 7.52
CHEMBL448727 Kd = 35.48 nM 7.45
CHEMBL51987 Kd = 41.69 nM 7.38
CHEMBL49573 Kd = 47.86 nM 7.32
CHEMBL49952 Kd = 47.86 nM 7.32
CHEMBL295935 Kd = 72.44 nM 7.14
CHEMBL50007 Kd = 74.13 nM 7.13
CHEMBL417910 Kd = 87.1 nM 7.06
CHEMBL422050 Kd = 97.72 nM 7.01
CHEMBL48868 Kd = 107.15 nM 6.97
CHEMBL48145 Kd = 114.82 nM 6.94
CHEMBL49587 Kd = 138.04 nM 6.86
CHEMBL49294 Kd = 151.36 nM 6.82
CHEMBL48400 Kd = 338.84 nM 6.47
CHEMBL49848 Kd = 776.25 nM 6.11
CHEMBL48259 Kd = 933.25 nM 6.03
CHEMBL48606 Kd > 100.0 nM -
CHEMBL299608 Kd > 100.0 nM -
CHEMBL48511 Kd > 100.0 nM -
CHEMBL421865 Kd > 100.0 nM -
CHEMBL50417 Kd > 100.0 nM -
CHEMBL52053 Kd > 100.0 nM -