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Assay Detail

CHEMBL648957

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

Binding
Inhibition of [125I]angiotensin II specific binding to rat mesenteric arteries
40
Total Activities
40
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

Imidazole-5-acrylic acids: potent nonpeptide angiotensin II receptor antagonists designed using a novel peptide pharmacophore model.
Keenan RM, Weinstock J, Finkelstein JA, Franz RG, Gaitanopoulos DE, Girard GR, Hill DT, Morgan TM, Samanen JM, Hempel J.
J Med Chem (1992) 35 : 3858 -3872
PubMed 1433195 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 5.44 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL125786 1 7.24
CHEMBL126594 1 6.92
CHEMBL339961 1 6.82
CHEMBL126356 1 6.60
CHEMBL339446 1 6.52
CHEMBL127005 1 6.44
CHEMBL338478 1 6.33
CHEMBL126359 1 6.09
CHEMBL339860 1 6.09
CHEMBL338517 1 6.09
CHEMBL127379 1 6.07
CHEMBL436594 1 5.92
CHEMBL444069 1 5.72
CHEMBL127308 1 5.54
CHEMBL126501 1 5.44
CHEMBL339623 1 5.34
CHEMBL338067 1 5.28
CHEMBL338249 1 5.17
CHEMBL405525 1 5.16
CHEMBL126500 1 5.05
CHEMBL338690 1 5.01
CHEMBL127916 1 4.92
CHEMBL339939 1 4.84
CHEMBL127515 1 4.78
CHEMBL127566 1 4.77
CHEMBL125341 1 4.73
CHEMBL127137 1 4.72
CHEMBL434254 1 4.70
CHEMBL435804 1 4.66
CHEMBL340433 1 4.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL125786 IC50 = 58.0 nM 7.24
CHEMBL126594 IC50 = 120.0 nM 6.92
CHEMBL339961 IC50 = 150.0 nM 6.82
CHEMBL126356 IC50 = 250.0 nM 6.60
CHEMBL339446 IC50 = 300.0 nM 6.52
CHEMBL127005 IC50 = 360.0 nM 6.44
CHEMBL338478 IC50 = 470.0 nM 6.33
CHEMBL126359 IC50 = 810.0 nM 6.09
CHEMBL339860 IC50 = 820.0 nM 6.09
CHEMBL338517 IC50 = 810.0 nM 6.09
CHEMBL127379 IC50 = 860.0 nM 6.07
CHEMBL436594 IC50 = 1200.0 nM 5.92
CHEMBL444069 IC50 = 1900.0 nM 5.72
CHEMBL127308 IC50 = 2900.0 nM 5.54
CHEMBL126501 IC50 = 3600.0 nM 5.44
CHEMBL339623 IC50 = 4600.0 nM 5.34
CHEMBL338067 IC50 = 5200.0 nM 5.28
CHEMBL338249 IC50 = 6800.0 nM 5.17
CHEMBL405525 IC50 = 6900.0 nM 5.16
CHEMBL126500 IC50 = 8900.0 nM 5.05
CHEMBL338690 IC50 = 9800.0 nM 5.01
CHEMBL127916 IC50 = 12000.0 nM 4.92
CHEMBL339939 IC50 = 14600.0 nM 4.84
CHEMBL127515 IC50 = 16500.0 nM 4.78
CHEMBL127566 IC50 = 17000.0 nM 4.77
CHEMBL125341 IC50 = 18700.0 nM 4.73
CHEMBL127137 IC50 = 19000.0 nM 4.72
CHEMBL434254 IC50 = 20100.0 nM 4.70
CHEMBL435804 IC50 = 21900.0 nM 4.66
CHEMBL340433 IC50 = 22000.0 nM 4.66
CHEMBL338423 IC50 = 22300.0 nM 4.65
CHEMBL126357 IC50 = 23500.0 nM 4.63
CHEMBL340316 IC50 = 28400.0 nM 4.55
CHEMBL339121 IC50 = 33900.0 nM 4.47
CHEMBL353234 IC50 = 38000.0 nM 4.42
CHEMBL420515 IC50 > 100000.0 nM -
CHEMBL340917 IC50 > 10000.0 nM -
CHEMBL291114 IC50 = 124000.0 nM -
CHEMBL2111841 IC50 > 100000.0 nM -
CHEMBL341011 IC50 = 127000.0 nM -