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Assay Detail

CHEMBL874236

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

Binding
Inhibition of partially purified soluble aminopeptidase from rat brain
23
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design of novel inhibitors of aminopeptidases. Synthesis of peptide-derived diamino thiols and sulfur replacement analogues of bestatin.
Gordon EM, Godfrey JD, Delaney NG, Asaad MM, Von Langen D, Cushman DW.
J Med Chem (1988) 31 : 2199 -2211
PubMed 3184127 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.67 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL302577 1 9.00
CHEMBL302135 1 8.40
CHEMBL448735 1 8.00
CHEMBL70366 2 7.70
CHEMBL68630 2 7.54
CHEMBL70509 1 7.48
CHEMBL308669 1 7.47
CHEMBL34907 1 7.41
CHEMBL29292 UBENIMEX 2.0 1 6.77
CHEMBL70725 2 6.66
CHEMBL303661 2 6.66
CHEMBL306968 1 6.24
CHEMBL70109 2 6.22
CHEMBL70875 1 5.80
CHEMBL421105 2 5.60
CHEMBL71681 1 5.16
CHEMBL420743 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL302577 IC50 = 1.0 nM 9.00
CHEMBL302135 IC50 = 4.0 nM 8.40
CHEMBL448735 IC50 = 10.0 nM 8.00
CHEMBL70366 IC50 = 20.0 nM 7.70
CHEMBL68630 IC50 = 29.0 nM 7.54
CHEMBL70509 IC50 = 33.0 nM 7.48
CHEMBL308669 IC50 = 34.0 nM 7.47
CHEMBL34907 IC50 = 39.0 nM 7.41
CHEMBL68630 IC50 = 81.0 nM 7.09
CHEMBL29292 UBENIMEX IC50 = 170.0 nM 6.77
CHEMBL70725 IC50 = 220.0 nM 6.66
CHEMBL303661 IC50 = 220.0 nM 6.66
CHEMBL70366 IC50 = 300.0 nM 6.52
CHEMBL306968 IC50 = 580.0 nM 6.24
CHEMBL70109 IC50 = 600.0 nM 6.22
CHEMBL70875 IC50 = 1600.0 nM 5.80
CHEMBL421105 IC50 = 2500.0 nM 5.60
CHEMBL70109 IC50 = 3100.0 nM 5.51
CHEMBL70725 IC50 = 4400.0 nM 5.36
CHEMBL71681 IC50 = 6900.0 nM 5.16
CHEMBL421105 IC50 = 7500.0 nM 5.12
CHEMBL303661 IC50 = 10000.0 nM 5.00
CHEMBL420743 IC50 = 240000.0 nM -