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Assay Detail

CHEMBL1948973

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

Binding
Inhibition of Mycobacterium tuberculosis PTP-A using p-nitrophenyl phosphate as substrate measured for 10 mins by spectrofluorimetry
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mycobacterium tuberculosis
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Low molecular weight protein-tyrosine phosphatase A (CHEMBL4542)
Type SINGLE PROTEIN
Organism Mycobacterium tuberculosis

Publication

Synthesis, biological evaluation, and molecular modeling of chalcone derivatives as potent inhibitors of Mycobacterium tuberculosis protein tyrosine phosphatases (PtpA and PtpB).
Chiaradia LD, Martins PG, Cordeiro MN, Guido RV, Ecco G, Andricopulo AD, Yunes RA, Vernal J, Nunes RJ, Terenzi H.
J Med Chem (2012) 55 : 390 -402
PubMed 22136336 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 4.20 4.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1945186 1 4.82
CHEMBL1946281 1 4.50
CHEMBL455469 1 4.35
CHEMBL455453 1 4.21
CHEMBL1946982 1 4.18
CHEMBL1946981 1 4.13
CHEMBL1946988 1 4.08
CHEMBL1945552 1 4.03
CHEMBL1098610 1 4.03
CHEMBL1946992 1 4.03
CHEMBL1946997 1 4.03
CHEMBL1946279 1 4.00
CHEMBL1945997 1 -
CHEMBL1945999 1 -
CHEMBL1946001 1 -
CHEMBL519069 1 -
CHEMBL1946280 1 -
CHEMBL1946282 1 -
CHEMBL1946285 1 -
CHEMBL1946439 1 -
CHEMBL1946440 1 -
CHEMBL1946984 1 -
CHEMBL1946985 1 -
CHEMBL1946986 1 -
CHEMBL1288972 1 -
CHEMBL1946990 1 -
CHEMBL1945185 1 -
CHEMBL1946993 1 -
CHEMBL1945187 1 -
CHEMBL1946998 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1945186 IC50 = 15000.0 nM 4.82
CHEMBL1946281 IC50 = 32000.0 nM 4.50
CHEMBL455469 IC50 = 45000.0 nM 4.35
CHEMBL455453 IC50 = 62000.0 nM 4.21
CHEMBL1946982 IC50 = 66000.0 nM 4.18
CHEMBL1946981 IC50 = 74000.0 nM 4.13
CHEMBL1946988 IC50 = 83000.0 nM 4.08
CHEMBL1946997 IC50 = 93000.0 nM 4.03
CHEMBL1946992 IC50 = 93000.0 nM 4.03
CHEMBL1098610 IC50 = 93000.0 nM 4.03
CHEMBL1945552 IC50 = 93000.0 nM 4.03
CHEMBL1946279 IC50 = 100000.0 nM 4.00
CHEMBL1945702 IC50 = 101000.0 nM -
CHEMBL1096287 IC50 - -
CHEMBL1945996 IC50 = 1023000.0 nM -
CHEMBL1945997 IC50 = 1659000.0 nM -
CHEMBL1945999 IC50 = 331000.0 nM -
CHEMBL1946001 IC50 - -
CHEMBL519069 IC50 > 50000.0 nM -
CHEMBL1946280 IC50 - -
CHEMBL1946282 IC50 = 302000.0 nM -
CHEMBL1946285 IC50 = 151000.0 nM -
CHEMBL1946439 IC50 - -
CHEMBL1946440 IC50 = 169000.0 nM -
CHEMBL1946984 IC50 = 155000.0 nM -
CHEMBL1946985 IC50 = 407000.0 nM -
CHEMBL1946986 IC50 = 174000.0 nM -
CHEMBL1288972 IC50 = 117000.0 nM -
CHEMBL1946990 IC50 - -
CHEMBL1945185 IC50 - -
CHEMBL1946993 IC50 = 214000.0 nM -
CHEMBL1945187 IC50 = 102000.0 nM -
CHEMBL1946998 IC50 > 100000.0 nM -