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Assay Detail

CHEMBL662806

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

Binding
Evaluated for inhibitory activity against Human fibroblast collagenase (HFC)
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Interstitial collagenase (CHEMBL332)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Relationship between structure and bioavailability in a series of hydroxamate based metalloprotease inhibitors
Singh J, Conzentino P, Cundy K, Gainor JA, Gilliam CL, Gordon TD, Johnson JA, Morgan BA, Schneider ED, Wahl RC, Whipple DA
Bioorg Med Chem Lett (1995) 5 : 337 -342
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 8.50 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL324947 1 9.00
CHEMBL114458 1 9.00
CHEMBL113894 1 8.70
CHEMBL19611 ILOMASTAT 2.0 1 8.70
CHEMBL116676 1 8.70
CHEMBL114094 1 8.70
CHEMBL332250 1 8.52
CHEMBL324140 1 8.52
CHEMBL325214 1 8.52
CHEMBL423876 1 8.52
CHEMBL430704 1 8.52
CHEMBL331355 1 8.40
CHEMBL324023 1 8.40
CHEMBL116507 1 8.30
CHEMBL114665 1 8.30
CHEMBL116972 1 8.30
CHEMBL280271 1 8.22
CHEMBL45483 1 8.22
CHEMBL117220 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL324947 Ki = 1.0 nM 9.00
CHEMBL114458 Ki = 1.0 nM 9.00
CHEMBL113894 Ki = 2.0 nM 8.70
CHEMBL19611 ILOMASTAT Ki = 2.0 nM 8.70
CHEMBL116676 Ki = 2.0 nM 8.70
CHEMBL114094 Ki = 2.0 nM 8.70
CHEMBL332250 Ki = 3.0 nM 8.52
CHEMBL324140 Ki = 3.0 nM 8.52
CHEMBL325214 Ki = 3.0 nM 8.52
CHEMBL423876 Ki = 3.0 nM 8.52
CHEMBL430704 Ki = 3.0 nM 8.52
CHEMBL331355 Ki = 4.0 nM 8.40
CHEMBL324023 Ki = 4.0 nM 8.40
CHEMBL116507 Ki = 5.0 nM 8.30
CHEMBL114665 Ki = 5.0 nM 8.30
CHEMBL116972 Ki = 5.0 nM 8.30
CHEMBL280271 Ki = 6.0 nM 8.22
CHEMBL45483 Ki = 6.0 nM 8.22
CHEMBL117220 Ki = 12.0 nM 7.92