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Assay Detail

CHEMBL4024807

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

Binding
Inhibition of IRAP (unknown origin) expressed in HEK 293S GnTI(-) cells by in vitro fluorimetric assay
31
Total Activities
31
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

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

Publication

Optimization and Structure-Activity Relationships of Phosphinic Pseudotripeptide Inhibitors of Aminopeptidases That Generate Antigenic Peptides.
Kokkala P, Mpakali A, Mauvais FX, Papakyriakou A, Daskalaki I, Petropoulou I, Kavvalou S, Papathanasopoulou M, Agrotis S, Fonsou TM, van Endert P, Stratikos E, Georgiadis D.
J Med Chem (2016) 59 : 9107 -9123
PubMed 27606717 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.18 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4101200 1 8.70
CHEMBL4095882 1 8.40
CHEMBL4077855 1 8.05
CHEMBL4099107 1 8.00
CHEMBL4081073 1 7.89
CHEMBL4080145 1 7.89
CHEMBL4089555 1 7.85
CHEMBL4069576 1 7.80
CHEMBL4069425 1 7.75
CHEMBL4104383 1 7.70
CHEMBL4094131 1 7.68
CHEMBL4097268 1 7.54
CHEMBL4081682 1 7.50
CHEMBL4065841 1 7.50
CHEMBL4103640 1 7.47
CHEMBL4099693 1 7.39
CHEMBL4085707 1 7.39
CHEMBL4074464 1 7.34
CHEMBL3416733 1 7.24
CHEMBL4091951 1 6.99
CHEMBL4077711 1 6.73
CHEMBL4096799 1 6.66
CHEMBL4073490 1 6.55
CHEMBL4086352 1 6.50
CHEMBL4066723 1 6.42
CHEMBL4096656 1 6.36
CHEMBL4093454 1 6.25
CHEMBL4064891 1 6.24
CHEMBL4070078 1 5.76
CHEMBL4088020 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4101200 IC50 = 2.0 nM 8.70
CHEMBL4095882 IC50 = 4.0 nM 8.40
CHEMBL4077855 IC50 = 9.0 nM 8.05
CHEMBL4099107 IC50 = 10.0 nM 8.00
CHEMBL4081073 IC50 = 13.0 nM 7.89
CHEMBL4080145 IC50 = 13.0 nM 7.89
CHEMBL4089555 IC50 = 14.0 nM 7.85
CHEMBL4069576 IC50 = 16.0 nM 7.80
CHEMBL4069425 IC50 = 18.0 nM 7.75
CHEMBL4104383 IC50 = 20.0 nM 7.70
CHEMBL4094131 IC50 = 21.0 nM 7.68
CHEMBL4097268 IC50 = 29.0 nM 7.54
CHEMBL4081682 IC50 = 32.0 nM 7.50
CHEMBL4065841 IC50 = 32.0 nM 7.50
CHEMBL4103640 IC50 = 34.0 nM 7.47
CHEMBL4099693 IC50 = 41.0 nM 7.39
CHEMBL4085707 IC50 = 41.0 nM 7.39
CHEMBL4074464 IC50 = 46.0 nM 7.34
CHEMBL3416733 IC50 = 57.0 nM 7.24
CHEMBL4091951 IC50 = 102.0 nM 6.99
CHEMBL4077711 IC50 = 185.0 nM 6.73
CHEMBL4096799 IC50 = 221.0 nM 6.66
CHEMBL4073490 IC50 = 281.0 nM 6.55
CHEMBL4086352 IC50 = 317.0 nM 6.50
CHEMBL4066723 IC50 = 381.0 nM 6.42
CHEMBL4096656 IC50 = 434.0 nM 6.36
CHEMBL4093454 IC50 = 561.0 nM 6.25
CHEMBL4064891 IC50 = 577.0 nM 6.24
CHEMBL4070078 IC50 = 1754.0 nM 5.76
CHEMBL4088020 IC50 = 1800.0 nM 5.75
CHEMBL4095735 IC50 = 4024.0 nM 5.39