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Assay Detail

CHEMBL873060

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Binding
Binding affinity against recombinant Aminopeptidase A
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glutamyl aminopeptidase (CHEMBL3439)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Investigation of subsite preferences in aminopeptidase A (EC 3.4.11.7) led to the design of the first highly potent and selective inhibitors of this enzyme.
David C, Bischoff L, Meudal H, Mothé A, De Mota N, DaNascimento S, Llorens-Cortes C, Fournié-Zaluski MC, Roques BP.
J Med Chem (1999) 42 : 5197 -5211
PubMed 10602705 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 7.37 9.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL146746 1 9.06
CHEMBL358903 1 8.49
CHEMBL348205 1 8.45
CHEMBL148777 1 8.44
CHEMBL151631 1 8.42
CHEMBL147285 1 8.37
CHEMBL359101 1 8.27
CHEMBL347763 1 8.03
CHEMBL356858 1 7.92
CHEMBL346397 1 7.89
CHEMBL433935 1 7.83
CHEMBL148482 1 7.82
CHEMBL146922 1 7.80
CHEMBL345941 1 7.70
CHEMBL151900 1 7.57
CHEMBL149449 1 7.40
CHEMBL148781 1 7.30
CHEMBL1161295 1 7.29
CHEMBL149436 1 7.28
CHEMBL357586 1 7.13
CHEMBL1161305 1 7.10
CHEMBL436269 1 7.08
CHEMBL357167 1 6.96
CHEMBL348192 1 6.84
CHEMBL1161304 1 6.82
CHEMBL151630 1 6.62
CHEMBL344321 1 6.57
CHEMBL149339 1 6.55
CHEMBL149145 1 6.54
CHEMBL147410 1 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL146746 Ki = 0.873 nM 9.06
CHEMBL358903 Ki = 3.2 nM 8.49
CHEMBL348205 Ki = 3.56 nM 8.45
CHEMBL148777 Ki = 3.6 nM 8.44
CHEMBL151631 Ki = 3.83 nM 8.42
CHEMBL147285 Ki = 4.3 nM 8.37
CHEMBL359101 Ki = 5.36 nM 8.27
CHEMBL347763 Ki = 9.3 nM 8.03
CHEMBL356858 Ki = 12.0 nM 7.92
CHEMBL346397 Ki = 13.0 nM 7.89
CHEMBL433935 Ki = 14.7 nM 7.83
CHEMBL148482 Ki = 15.0 nM 7.82
CHEMBL146922 Ki = 16.0 nM 7.80
CHEMBL345941 Ki = 20.0 nM 7.70
CHEMBL151900 Ki = 27.0 nM 7.57
CHEMBL149449 Ki = 40.0 nM 7.40
CHEMBL148781 Ki = 50.0 nM 7.30
CHEMBL1161295 Ki = 51.0 nM 7.29
CHEMBL149436 Ki = 53.0 nM 7.28
CHEMBL357586 Ki = 73.3 nM 7.13
CHEMBL1161305 Ki = 80.0 nM 7.10
CHEMBL436269 Ki = 83.3 nM 7.08
CHEMBL357167 Ki = 110.0 nM 6.96
CHEMBL348192 Ki = 145.0 nM 6.84
CHEMBL1161304 Ki = 150.0 nM 6.82
CHEMBL151630 Ki = 240.0 nM 6.62
CHEMBL344321 Ki = 267.0 nM 6.57
CHEMBL149339 Ki = 283.0 nM 6.55
CHEMBL149145 Ki = 292.0 nM 6.54
CHEMBL147410 Ki = 470.0 nM 6.33
CHEMBL149947 Ki = 910.0 nM 6.04
CHEMBL148746 Ki = 1200.0 nM 5.92
CHEMBL146911 Ki = 4200.0 nM 5.38