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Assay Detail

CHEMBL4710796

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

Binding
Inhibition of beta-lactamase IMP-1 (unknown origin) expressed in Escherichia coli BL21(DE3) using imipenem as substrate by measuring substrate hydrolysis by spectrophotometric analysis
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Not specified
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

4-Amino-1,2,4-triazole-3-thione-derived Schiff bases as metallo-β-lactamase inhibitors.
Gavara L,Sevaille L,De Luca F,Mercuri P,Bebrone C,Feller G,Legru A,Cerboni G,Tanfoni S,Baud D,Cutolo G,Bestgen B,Chelini G,Verdirosa F,Sannio F,Pozzi C,Benvenuti M,Kwapien K,Fischer M,Becker K,Frère JM,Mangani S,Gresh N,Berthomieu D,Galleni M,Docquier JD,Hernandez JF
Eur J Med Chem (2020) 208 : 112720 -112720
PubMed 32937203 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 5.10 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4754134 1 7.00
CHEMBL4796301 1 7.00
CHEMBL4758987 1 6.52
CHEMBL4751964 1 5.66
CHEMBL4760501 1 5.52
CHEMBL4780392 1 5.05
CHEMBL4763927 1 5.05
CHEMBL4758368 1 5.05
CHEMBL4776119 1 5.05
CHEMBL4778216 1 5.00
CHEMBL4754312 1 4.97
CHEMBL4785513 1 4.96
CHEMBL4779391 1 4.96
CHEMBL4789945 1 4.96
CHEMBL4746528 1 4.94
CHEMBL4757595 1 4.92
CHEMBL4798128 1 4.75
CHEMBL4760444 1 4.49
CHEMBL4749729 1 4.46
CHEMBL4792428 1 4.26
CHEMBL4797119 1 4.24
CHEMBL4790117 1 4.24
CHEMBL4778397 1 4.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4754134 Ki = 100.0 nM 7.00
CHEMBL4796301 Ki = 100.0 nM 7.00
CHEMBL4758987 Ki = 300.0 nM 6.52
CHEMBL4751964 Ki = 2200.0 nM 5.66
CHEMBL4760501 Ki = 3000.0 nM 5.52
CHEMBL4780392 Ki = 9000.0 nM 5.05
CHEMBL4763927 Ki = 9000.0 nM 5.05
CHEMBL4758368 Ki = 9000.0 nM 5.05
CHEMBL4776119 Ki = 9000.0 nM 5.05
CHEMBL4778216 Ki = 10000.0 nM 5.00
CHEMBL4754312 Ki = 10600.0 nM 4.97
CHEMBL4785513 Ki = 11000.0 nM 4.96
CHEMBL4779391 Ki = 11000.0 nM 4.96
CHEMBL4789945 Ki = 11000.0 nM 4.96
CHEMBL4746528 Ki = 11400.0 nM 4.94
CHEMBL4757595 Ki = 12000.0 nM 4.92
CHEMBL4798128 Ki = 17700.0 nM 4.75
CHEMBL4760444 Ki = 32400.0 nM 4.49
CHEMBL4749729 Ki = 34400.0 nM 4.46
CHEMBL4792428 Ki = 54700.0 nM 4.26
CHEMBL4797119 Ki = 58000.0 nM 4.24
CHEMBL4790117 Ki = 58000.0 nM 4.24
CHEMBL4778397 Ki = 66200.0 nM 4.18