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Assay Detail

CHEMBL2329965

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

Binding
Inhibition of human recombinant IDE-mediated FRET1 degradation
20
Total Activities
20
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

Insulin-degrading enzyme (CHEMBL1293287)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of peptide hydroxamate inhibitors of insulin-degrading enzyme reveals marked substrate-selectivity.
Abdul-Hay SO, Lane AL, Caulfield TR, Claussin C, Bertrand J, Masson A, Choudhry S, Fauq AH, Maharvi GM, Leissring MA.
J Med Chem (2013) 56 : 2246 -2255
PubMed 23437776 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 6.64 8.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2324220 1 8.53
CHEMBL2324207 1 7.64
CHEMBL2324201 1 7.59
CHEMBL2324206 1 7.36
CHEMBL2324204 1 7.30
CHEMBL2324209 1 7.13
CHEMBL2324219 1 7.11
CHEMBL2324205 1 7.07
CHEMBL2324203 1 7.06
CHEMBL2324202 1 6.99
CHEMBL2324213 1 6.30
CHEMBL2324208 1 5.94
CHEMBL2324218 1 5.28
CHEMBL2324214 1 5.15
CHEMBL2324212 1 5.11
CHEMBL2324211 1 4.75
CHEMBL2324210 1 -
CHEMBL2324215 1 -
CHEMBL2324216 1 -
CHEMBL2324217 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2324220 Ki = 2.96 nM 8.53
CHEMBL2324207 Ki = 23.1 nM 7.64
CHEMBL2324201 Ki = 25.9 nM 7.59
CHEMBL2324206 Ki = 43.7 nM 7.36
CHEMBL2324204 Ki = 49.8 nM 7.30
CHEMBL2324209 Ki = 73.3 nM 7.13
CHEMBL2324219 Ki = 78.0 nM 7.11
CHEMBL2324205 Ki = 85.1 nM 7.07
CHEMBL2324203 Ki = 87.0 nM 7.06
CHEMBL2324202 Ki = 103.0 nM 6.99
CHEMBL2324213 Ki = 498.0 nM 6.30
CHEMBL2324208 Ki = 1150.0 nM 5.94
CHEMBL2324218 Ki = 5280.0 nM 5.28
CHEMBL2324214 Ki = 7020.0 nM 5.15
CHEMBL2324212 Ki = 7750.0 nM 5.11
CHEMBL2324211 Ki = 18000.0 nM 4.75
CHEMBL2324210 Ki > 33000.0 nM -
CHEMBL2324215 Ki > 33000.0 nM -
CHEMBL2324216 Ki > 33000.0 nM -
CHEMBL2324217 Ki > 33000.0 nM -