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Assay Detail

CHEMBL4407167

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Binding
Inhibition of soluble human APN ectodomain stably expressed in HEK293 GnTI(-) cells using H-Leu-NHMec as substrate preincubated for 10 mins followed by substrate addition and measured for 1 hr by spectrofluorimetric method
ChEMBL ↗
49
Total Activities
49
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

Novel Human Aminopeptidase N Inhibitors: Discovery and Optimization of Subsite Binding Interactions.
Lee J, Vinh NB, Drinkwater N, Yang W, Kannan Sivaraman K, Schembri LS, Gazdik M, Grin PM, Butler GS, Overall CM, Charman SA, McGowan S, Scammells PJ.
J Med Chem (2019) 62 : 7185 -7209
PubMed 31251594 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 49 6.74 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4460082 — — 1 8.35
CHEMBL4448936 — — 1 8.09
CHEMBL4445188 — — 1 7.72
CHEMBL4566015 — — 1 7.63
CHEMBL4522953 — — 1 7.54
CHEMBL4590563 — — 1 7.43
CHEMBL4578880 — — 1 7.40
CHEMBL4544937 — — 1 7.37
CHEMBL4589359 — — 1 7.31
CHEMBL4455419 — — 1 7.15
CHEMBL4586845 — — 1 7.09
CHEMBL4441367 — — 1 6.99
CHEMBL4446709 — — 1 6.96
CHEMBL3765455 — — 1 6.93
CHEMBL4572202 — — 1 6.92
CHEMBL4435512 — — 1 6.88
CHEMBL4588933 — — 1 6.86
CHEMBL4554326 — — 1 6.86
CHEMBL4593147 — — 1 6.81
CHEMBL4537181 — — 1 6.80
CHEMBL4462042 — — 1 6.79
CHEMBL4564549 — — 1 6.77
CHEMBL4579696 — — 1 6.76
CHEMBL4459712 — — 1 6.76
CHEMBL4566082 — — 1 6.74
CHEMBL4475350 — — 1 6.73
CHEMBL4462406 — — 1 6.73
CHEMBL4439556 — — 1 6.69
CHEMBL4468609 — — 1 6.63
CHEMBL4535765 — — 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4460082 — Ki = 4.5 nM 8.35
CHEMBL4448936 — Ki = 8.2 nM 8.09
CHEMBL4445188 — Ki = 19.2 nM 7.72
CHEMBL4566015 — Ki = 23.4 nM 7.63
CHEMBL4522953 — Ki = 29.1 nM 7.54
CHEMBL4590563 — Ki = 37.3 nM 7.43
CHEMBL4578880 — Ki = 40.0 nM 7.40
CHEMBL4544937 — Ki = 43.1 nM 7.37
CHEMBL4589359 — Ki = 49.1 nM 7.31
CHEMBL4455419 — Ki = 71.2 nM 7.15
CHEMBL4586845 — Ki = 82.1 nM 7.09
CHEMBL4441367 — Ki = 102.0 nM 6.99
CHEMBL4446709 — Ki = 111.0 nM 6.96
CHEMBL3765455 — Ki = 118.0 nM 6.93
CHEMBL4572202 — Ki = 119.0 nM 6.92
CHEMBL4435512 — Ki = 131.0 nM 6.88
CHEMBL4588933 — Ki = 138.0 nM 6.86
CHEMBL4554326 — Ki = 137.0 nM 6.86
CHEMBL4593147 — Ki = 156.0 nM 6.81
CHEMBL4537181 — Ki = 158.0 nM 6.80
CHEMBL4462042 — Ki = 163.0 nM 6.79
CHEMBL4564549 — Ki = 170.0 nM 6.77
CHEMBL4579696 — Ki = 175.0 nM 6.76
CHEMBL4459712 — Ki = 172.0 nM 6.76
CHEMBL4566082 — Ki = 182.0 nM 6.74
CHEMBL4462406 — Ki = 185.0 nM 6.73
CHEMBL4475350 — Ki = 188.0 nM 6.73
CHEMBL4439556 — Ki = 205.0 nM 6.69
CHEMBL4468609 — Ki = 235.0 nM 6.63
CHEMBL4535765 — Ki = 240.0 nM 6.62
CHEMBL4440454 — Ki = 277.0 nM 6.56
CHEMBL4460369 — Ki = 348.0 nM 6.46
CHEMBL4562848 — Ki = 366.0 nM 6.44
CHEMBL4442426 — Ki = 430.0 nM 6.37
CHEMBL4440320 — Ki = 442.0 nM 6.36
CHEMBL4531395 — Ki = 462.0 nM 6.33
CHEMBL4458367 — Ki = 497.0 nM 6.30
CHEMBL4540925 — Ki = 522.0 nM 6.28
CHEMBL4467963 — Ki = 560.0 nM 6.25
CHEMBL4439575 — Ki = 604.0 nM 6.22
CHEMBL4586126 — Ki = 631.0 nM 6.20
CHEMBL4445018 — Ki = 704.0 nM 6.15
CHEMBL4454625 — Ki = 745.0 nM 6.13
CHEMBL4571223 — Ki = 919.0 nM 6.04
CHEMBL4446876 — Ki = 978.0 nM 6.01
CHEMBL2103847 TOSEDOSTAT Ki = 1180.0 nM 5.93
CHEMBL29292 UBENIMEX Ki = 2370.0 nM 5.62
CHEMBL4564908 — Ki = 4420.0 nM 5.36
CHEMBL4439004 — Ki > 1000000.0 nM -