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Assay Detail

CHEMBL3419982

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

Binding
Inhibition of human recombinant IRAP expressed in baculovirus infected cabbage looper ovary Hi5 cells using L-leucine-7-amido-4-methyl coumarin as substrate after 5 to 10 mins by fluorescence assay
ChEMBL ↗
68
Total Activities
68
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Female gonad
Cell Type BTI-TN-5B1-4
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Leucyl-cystinyl aminopeptidase (CHEMBL2693) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3,4-diaminobenzoic acid derivatives as inhibitors of the oxytocinase subfamily of M1 aminopeptidases with immune-regulating properties.
Papakyriakou A, Zervoudi E, Tsoukalidou S, Mauvais FX, Sfyroera G, Mastellos DC, van Endert P, Theodorakis EA, Vourloumis D, Stratikos E.
J Med Chem (2015) 58 : 1524 -1543
PubMed 25635706 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 68 5.33 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3416733 — — 1 7.52
CHEMBL3416692 — — 1 6.98
CHEMBL3416693 — — 1 6.53
CHEMBL3416726 — — 1 6.36
CHEMBL3416697 — — 1 6.18
CHEMBL3416687 — — 1 6.03
CHEMBL3416696 — — 1 6.01
CHEMBL3416691 — — 1 5.92
CHEMBL3416717 — — 1 5.89
CHEMBL3416711 — — 1 5.89
CHEMBL3416689 — — 1 5.89
CHEMBL3416698 — — 1 5.77
CHEMBL3416727 — — 1 5.77
CHEMBL3416568 — — 1 5.68
CHEMBL3416729 — — 1 5.66
CHEMBL3416712 — — 1 5.62
CHEMBL3416707 — — 1 5.60
CHEMBL3416714 — — 1 5.54
CHEMBL3416701 — — 1 5.48
CHEMBL3416695 — — 1 5.48
CHEMBL3416719 — — 1 5.47
CHEMBL3416725 — — 1 5.44
CHEMBL3416721 — — 1 5.43
CHEMBL3416715 — — 1 5.43
CHEMBL3416577 — — 1 5.42
CHEMBL3416716 — — 1 5.42
CHEMBL3416723 — — 1 5.41
CHEMBL3416583 — — 1 5.39
CHEMBL3416688 — — 1 5.36
CHEMBL3416713 — — 1 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3416733 — IC50 = 30.0 nM 7.52
CHEMBL3416692 — IC50 = 105.0 nM 6.98
CHEMBL3416693 — IC50 = 296.0 nM 6.53
CHEMBL3416726 — IC50 = 438.0 nM 6.36
CHEMBL3416697 — IC50 = 655.0 nM 6.18
CHEMBL3416687 — IC50 = 933.0 nM 6.03
CHEMBL3416696 — IC50 = 966.0 nM 6.01
CHEMBL3416691 — IC50 = 1200.0 nM 5.92
CHEMBL3416717 — IC50 = 1300.0 nM 5.89
CHEMBL3416711 — IC50 = 1300.0 nM 5.89
CHEMBL3416689 — IC50 = 1300.0 nM 5.89
CHEMBL3416698 — IC50 = 1700.0 nM 5.77
CHEMBL3416727 — IC50 = 1700.0 nM 5.77
CHEMBL3416568 — IC50 = 2100.0 nM 5.68
CHEMBL3416729 — IC50 = 2200.0 nM 5.66
CHEMBL3416712 — IC50 = 2400.0 nM 5.62
CHEMBL3416707 — IC50 = 2500.0 nM 5.60
CHEMBL3416714 — IC50 = 2900.0 nM 5.54
CHEMBL3416701 — IC50 = 3300.0 nM 5.48
CHEMBL3416695 — IC50 = 3300.0 nM 5.48
CHEMBL3416719 — IC50 = 3400.0 nM 5.47
CHEMBL3416725 — IC50 = 3600.0 nM 5.44
CHEMBL3416721 — IC50 = 3700.0 nM 5.43
CHEMBL3416715 — IC50 = 3700.0 nM 5.43
CHEMBL3416716 — IC50 = 3800.0 nM 5.42
CHEMBL3416577 — IC50 = 3800.0 nM 5.42
CHEMBL3416723 — IC50 = 3900.0 nM 5.41
CHEMBL3416583 — IC50 = 4100.0 nM 5.39
CHEMBL3416688 — IC50 = 4400.0 nM 5.36
CHEMBL3416713 — IC50 = 4700.0 nM 5.33
CHEMBL3416578 — IC50 = 4800.0 nM 5.32
CHEMBL3416731 — IC50 = 4900.0 nM 5.31
CHEMBL3416720 — IC50 = 5200.0 nM 5.28
CHEMBL3416580 — IC50 = 5700.0 nM 5.24
CHEMBL3416685 — IC50 = 7100.0 nM 5.15
CHEMBL3416572 — IC50 = 7200.0 nM 5.14
CHEMBL3416730 — IC50 = 7600.0 nM 5.12
CHEMBL3416699 — IC50 = 8300.0 nM 5.08
CHEMBL3416564 — IC50 = 10000.0 nM 5.00
CHEMBL3416704 — IC50 = 9900.0 nM 5.00
CHEMBL3416565 — IC50 = 10700.0 nM 4.97
CHEMBL3416579 — IC50 = 10700.0 nM 4.97
CHEMBL3416567 — IC50 = 10900.0 nM 4.96
CHEMBL3416569 — IC50 = 12000.0 nM 4.92
CHEMBL3416586 — IC50 = 12000.0 nM 4.92
CHEMBL3416709 — IC50 = 14400.0 nM 4.84
CHEMBL3416573 — IC50 = 14600.0 nM 4.84
CHEMBL3416710 — IC50 = 20200.0 nM 4.70
CHEMBL3416708 — IC50 = 20600.0 nM 4.69
CHEMBL3416588 — IC50 = 22000.0 nM 4.66