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Assay Detail

CHEMBL1799221

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Binding
Inhibition of Enterobacter cloacae beta lactamase P99
12
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Enterobacter cloacae
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-lactamase (CHEMBL2725)
Type SINGLE PROTEIN
Organism Enterobacter cloacae

Publication

Thiophenyl oxime-derived phosphonates as nano-molar class C beta-lactamase inhibitors reducing MIC of imipenem against Pseudomonas aeruginosa and Acinetobacter baumannii.
Tan Q, Ogawa AM, Raghoobar SL, Wisniewski D, Colwell L, Park YW, Young K, Hermes JD, Dininno FP, Hammond ML.
Bioorg Med Chem Lett (2011) 21 : 4363 -4365
PubMed 21664132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.62 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1795572 1 7.72
CHEMBL1795567 1 7.50
CHEMBL1795565 1 7.41
CHEMBL1795571 2 7.06
CHEMBL1795566 1 7.00
CHEMBL1795568 1 7.00
CHEMBL1795564 2 6.47
CHEMBL1795563 1 6.10
CHEMBL1795570 1 5.52
CHEMBL1795569 1 4.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1795572 IC50 = 19.0 nM 7.72
CHEMBL1795567 IC50 = 32.0 nM 7.50
CHEMBL1795565 IC50 = 39.0 nM 7.41
CHEMBL1795571 IC50 = 87.0 nM 7.06
CHEMBL1795566 IC50 = 100.0 nM 7.00
CHEMBL1795568 IC50 = 100.0 nM 7.00
CHEMBL1795571 IC50 = 170.0 nM 6.77
CHEMBL1795564 IC50 = 340.0 nM 6.47
CHEMBL1795564 IC50 = 710.0 nM 6.15
CHEMBL1795563 IC50 = 800.0 nM 6.10
CHEMBL1795570 IC50 = 3000.0 nM 5.52
CHEMBL1795569 IC50 = 21000.0 nM 4.68