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Assay Detail

CHEMBL4822041

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Binding
Inhibition of APN (unknown origin) using A-AMC as substrate
12
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Aminopeptidase N (CHEMBL1907)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Investigating the phosphinic acid tripeptide mimetic DG013A as a tool compound inhibitor of the M1-aminopeptidase ERAP1.
Wilding B, Pasqua AE, E A Chessum N, Pierrat OA, Hahner T, Tomlin K, Shehu E, Burke R, Richards GM, Whitton B, Arwert EN, Thapaliya A, Salimraj R, van Montfort R, Skawinska A, Hayes A, Raynaud F, Chopra R, Jones K, Newton G, Cheeseman MD.
Bioorg Med Chem Lett (2021) 42 : 128050 -128050
PubMed 33887439 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.68 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4854733 2 8.82
CHEMBL4877339 2 8.64
CHEMBL3416733 2 8.44
CHEMBL4853049 2 8.07
CHEMBL4863168 2 6.65
CHEMBL4872604 2 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4854733 IC50 = 1.5 nM 8.82
CHEMBL4854733 IC50 = 1.549 nM 8.81
CHEMBL4877339 IC50 = 2.291 nM 8.64
CHEMBL4877339 IC50 = 2.3 nM 8.64
CHEMBL3416733 IC50 = 3.631 nM 8.44
CHEMBL3416733 IC50 = 3.7 nM 8.43
CHEMBL4853049 IC50 = 8.6 nM 8.07
CHEMBL4853049 IC50 = 8.71 nM 8.06
CHEMBL4863168 IC50 = 223.87 nM 6.65
CHEMBL4863168 IC50 = 230.0 nM 6.64
CHEMBL4872604 IC50 = 3388.44 nM 5.47
CHEMBL4872604 IC50 = 3400.0 nM 5.47