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Assay Detail

CHEMBL936433

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

Binding
Inhibition of human recombinant IRAP expressed in HEK293 cells
18
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Beta-homo-amino acid scan of angiotensin IV.
Lukaszuk A, Demaegdt H, Szemenyei E, Tóth G, Tymecka D, Misicka A, Karoyan P, Vanderheyden P, Vauquelin G, Tourwé D.
J Med Chem (2008) 51 : 2291 -2296
PubMed 18386881 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.58 7.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL408871 1 7.69
CHEMBL259019 1 7.56
CHEMBL261120 ANGIOTENSIN IV 1 7.25
CHEMBL248592 1 7.09
CHEMBL260622 1 7.00
CHEMBL408132 1 6.96
CHEMBL261417 1 6.84
CHEMBL261731 1 6.83
CHEMBL261422 1 6.78
CHEMBL259382 1 6.76
CHEMBL428457 2 6.75
CHEMBL403717 1 6.20
CHEMBL427940 1 5.97
CHEMBL258480 1 5.88
CHEMBL258642 1 5.67
CHEMBL258452 1 5.27
CHEMBL258494 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL408871 Ki = 20.42 nM 7.69
CHEMBL259019 Ki = 27.54 nM 7.56
CHEMBL261120 ANGIOTENSIN IV Ki = 56.23 nM 7.25
CHEMBL248592 Ki = 81.28 nM 7.09
CHEMBL260622 Ki = 100.0 nM 7.00
CHEMBL408132 Ki = 109.65 nM 6.96
CHEMBL261417 Ki = 144.54 nM 6.84
CHEMBL261731 Ki = 147.91 nM 6.83
CHEMBL261422 Ki = 165.96 nM 6.78
CHEMBL259382 Ki = 173.78 nM 6.76
CHEMBL428457 Ki = 177.83 nM 6.75
CHEMBL428457 Ki = 199.53 nM 6.70
CHEMBL403717 Ki = 630.96 nM 6.20
CHEMBL427940 Ki = 1071.52 nM 5.97
CHEMBL258480 Ki = 1318.26 nM 5.88
CHEMBL258642 Ki = 2137.96 nM 5.67
CHEMBL258452 Ki = 5370.32 nM 5.27
CHEMBL258494 Ki = 5754.4 nM 5.24