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Assay Detail

CHEMBL3373423

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

Binding
Inhibition of pig recombinant alanyl aminopeptidase after 30 to 60 mins by morrison's equation
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Aminopeptidase N (CHEMBL2590)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Structure-guided, single-point modifications in the phosphinic dipeptide structure yield highly potent and selective inhibitors of neutral aminopeptidases.
Vassiliou S, Węglarz-Tomczak E, Berlicki Ł, Pawełczak M, Nocek B, Mulligan R, Joachimiak A, Mucha A.
J Med Chem (2014) 57 : 8140 -8151
PubMed 25192493 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.51 8.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL289824 1 8.91
CHEMBL3355110 1 8.82
CHEMBL3355111 1 8.41
CHEMBL1090914 1 8.40
CHEMBL3355099 1 8.39
CHEMBL3355109 1 8.38
CHEMBL3355108 1 7.77
CHEMBL3355105 1 7.72
CHEMBL3355106 1 7.64
CHEMBL88808 1 7.44
CHEMBL3355104 1 7.38
CHEMBL40422 LEUCINE PHOSPHONIC ACID 1 7.28
CHEMBL3355101 1 7.16
CHEMBL3355100 1 6.81
CHEMBL288165 1 6.72
CHEMBL3355103 1 6.68
CHEMBL327844 1 6.56
CHEMBL3355102 1 6.15
CHEMBL3355107 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL289824 Ki = 1.22 nM 8.91
CHEMBL3355110 Ki = 1.5 nM 8.82
CHEMBL3355111 Ki = 3.9 nM 8.41
CHEMBL1090914 Ki = 3.96 nM 8.40
CHEMBL3355099 Ki = 4.08 nM 8.39
CHEMBL3355109 Ki = 4.2 nM 8.38
CHEMBL3355108 Ki = 17.0 nM 7.77
CHEMBL3355105 Ki = 19.0 nM 7.72
CHEMBL3355106 Ki = 23.0 nM 7.64
CHEMBL88808 Ki = 36.0 nM 7.44
CHEMBL3355104 Ki = 42.0 nM 7.38
CHEMBL40422 LEUCINE PHOSPHONIC ACID Ki = 53.0 nM 7.28
CHEMBL3355101 Ki = 69.0 nM 7.16
CHEMBL3355100 Ki = 155.0 nM 6.81
CHEMBL288165 Ki = 192.0 nM 6.72
CHEMBL3355103 Ki = 208.0 nM 6.68
CHEMBL327844 Ki = 276.0 nM 6.56
CHEMBL3355102 Ki = 713.0 nM 6.15
CHEMBL3355107 Ki = 740.0 nM 6.13