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Assay Detail

CHEMBL648762

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Binding
Inhibitory concentration that gives 50% displacement of specific binding at labeled angiotensin II type 1 receptor in rat adrenal cortical membranes.
ChEMBL ↗
50
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Angiotensin II receptor (AT-1) type-1 (CHEMBL2094250) ↗
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Non-peptide angiotensin II receptor antagonists: chemical feature based pharmacophore identification.
Krovat EM, Langer T.
J Med Chem (2003) 46 : 716 -726
PubMed 12593652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 6.21 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL907 CARBOXYLIC ACID METABOLITE — 1 8.89
CHEMBL315094 — — 1 7.92
CHEMBL284425 — — 1 7.92
CHEMBL85692 — — 1 7.72
CHEMBL191 LOSARTAN 4.0 1 7.72
CHEMBL313715 — — 1 7.70
CHEMBL87755 — — 1 7.54
CHEMBL276956 — — 1 7.38
CHEMBL163342 — — 1 7.10
CHEMBL85984 — — 1 7.10
CHEMBL86041 — — 2 7.08
CHEMBL164363 — — 1 7.04
CHEMBL314673 — — 1 7.00
CHEMBL274447 — — 2 7.00
CHEMBL262958 — — 1 6.85
CHEMBL351835 — — 2 6.82
CHEMBL85601 — — 1 6.72
CHEMBL162802 — — 1 6.66
CHEMBL163760 — — 1 6.58
CHEMBL349667 — — 1 6.47
CHEMBL163766 — — 1 6.40
CHEMBL24512 — — 1 6.30
CHEMBL85435 — — 1 6.29
CHEMBL164215 — — 1 6.22
CHEMBL420778 — — 1 6.16
CHEMBL24934 — — 1 6.10
CHEMBL27216 — — 1 6.04
CHEMBL160004 — — 1 5.92
CHEMBL351674 — — 1 5.92
CHEMBL2114348 — — 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL907 CARBOXYLIC ACID METABOLITE IC50 = 1.3 nM 8.89
CHEMBL315094 — IC50 = 12.0 nM 7.92
CHEMBL284425 — IC50 = 12.0 nM 7.92
CHEMBL85692 — IC50 = 19.0 nM 7.72
CHEMBL191 LOSARTAN IC50 = 19.0 nM 7.72
CHEMBL313715 — IC50 = 20.0 nM 7.70
CHEMBL87755 — IC50 = 29.0 nM 7.54
CHEMBL276956 — IC50 = 42.0 nM 7.38
CHEMBL85984 — IC50 = 80.0 nM 7.10
CHEMBL163342 — IC50 = 80.0 nM 7.10
CHEMBL86041 — IC50 = 83.0 nM 7.08
CHEMBL164363 — IC50 = 92.0 nM 7.04
CHEMBL314673 — IC50 = 99.0 nM 7.00
CHEMBL274447 — IC50 = 99.0 nM 7.00
CHEMBL262958 — IC50 = 140.0 nM 6.85
CHEMBL351835 — IC50 = 150.0 nM 6.82
CHEMBL86041 — IC50 = 160.0 nM 6.80
CHEMBL85601 — IC50 = 190.0 nM 6.72
CHEMBL162802 — IC50 = 220.0 nM 6.66
CHEMBL351835 — IC50 = 230.0 nM 6.64
CHEMBL163760 — IC50 = 260.0 nM 6.58
CHEMBL349667 — IC50 = 340.0 nM 6.47
CHEMBL163766 — IC50 = 400.0 nM 6.40
CHEMBL24512 — IC50 = 500.0 nM 6.30
CHEMBL85435 — IC50 = 510.0 nM 6.29
CHEMBL164215 — IC50 = 600.0 nM 6.22
CHEMBL420778 — IC50 = 700.0 nM 6.16
CHEMBL24934 — IC50 = 790.0 nM 6.10
CHEMBL27216 — IC50 = 920.0 nM 6.04
CHEMBL351674 — IC50 = 1200.0 nM 5.92
CHEMBL160004 — IC50 = 1200.0 nM 5.92
CHEMBL2114348 — IC50 = 1700.0 nM 5.77
CHEMBL285353 — IC50 = 2400.0 nM 5.62
CHEMBL348816 — IC50 = 2800.0 nM 5.55
CHEMBL27280 — IC50 = 2900.0 nM 5.54
CHEMBL315386 — IC50 = 3330.0 nM 5.48
CHEMBL84111 — IC50 = 4100.0 nM 5.39
CHEMBL350503 — IC50 = 5800.0 nM 5.24
CHEMBL420048 — IC50 = 6300.0 nM 5.20
CHEMBL274447 — IC50 = 11000.0 nM 4.96
CHEMBL313324 — IC50 = 11000.0 nM 4.96
CHEMBL25574 — IC50 = 13000.0 nM 4.89
CHEMBL284426 — IC50 = 13000.0 nM 4.89
CHEMBL25686 — IC50 = 19000.0 nM 4.72
CHEMBL416384 — IC50 = 28000.0 nM 4.55
CHEMBL25574 — IC50 = 32000.0 nM 4.50
CHEMBL279683 — IC50 = 32000.0 nM 4.50
CHEMBL280800 — IC50 = 46000.0 nM 4.34
CHEMBL416384 — IC50 = 100000.0 nM 4.00
CHEMBL279683 — IC50 = 150000.0 nM -