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Assay Detail

CHEMBL4843584

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

Binding
Inhibition of PREP (unknown origin) using fluorogenic substrate by spectrometric assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structure-activity relationship and biochemical evaluation of novel fibroblast activation protein and prolyl endopeptidase inhibitors with α-ketoamide warheads.
Šimková A, Ormsby T, Sidej N, Slavětínská LP, Brynda J, Beranová J, Šácha P, Majer P, Konvalinka J.
Eur J Med Chem (2021) 224 : 113717 -113717
PubMed 34371463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.91 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4877950 1 9.62
CHEMBL4864133 1 9.59
CHEMBL4876026 1 9.54
CHEMBL4854865 1 9.44
CHEMBL4855449 1 9.40
CHEMBL4853661 1 9.37
CHEMBL4868869 1 9.31
CHEMBL4878759 1 9.28
CHEMBL4859756 1 9.18
CHEMBL4871602 1 9.14
CHEMBL4864489 1 8.89
CHEMBL3233842 1 6.51
CHEMBL2385281 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4877950 IC50 = 0.24 nM 9.62
CHEMBL4864133 IC50 = 0.26 nM 9.59
CHEMBL4876026 IC50 = 0.29 nM 9.54
CHEMBL4854865 IC50 = 0.36 nM 9.44
CHEMBL4855449 IC50 = 0.4 nM 9.40
CHEMBL4853661 IC50 = 0.43 nM 9.37
CHEMBL4868869 IC50 = 0.49 nM 9.31
CHEMBL4878759 IC50 = 0.53 nM 9.28
CHEMBL4859756 IC50 = 0.66 nM 9.18
CHEMBL4871602 IC50 = 0.73 nM 9.14
CHEMBL4864489 IC50 = 1.3 nM 8.89
CHEMBL3233842 IC50 = 310.0 nM 6.51
CHEMBL2385281 IC50 = 320.0 nM 6.50