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Assay Detail

CHEMBL4265149

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

Binding
Inhibition of recombinant Mycobacterium tuberculosis PtpA using p-nitrophenyl phosphate as substrate preincubated for 10 mins followed by substrate addition and measured every minute for 10 mins by UV-VIS spectrophotometric analysis
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthetic thiosemicarbazones as a new class of Mycobacterium tuberculosis protein tyrosine phosphatase A inhibitors.
Sens L, de Souza ACA, Pacheco LA, Menegatti ACO, Mori M, Mascarello A, Nunes RJ, Terenzi H.
Bioorg Med Chem (2018) 26 : 5742 -5750
PubMed 30389409 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 4.95 5.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4288744 1 5.54
CHEMBL4280516 1 5.13
CHEMBL4282817 1 5.04
CHEMBL4292242 1 5.02
CHEMBL4279400 1 4.87
CHEMBL4294511 1 4.82
CHEMBL4280931 1 4.75
CHEMBL4285399 1 4.74
CHEMBL4287324 1 4.62
CHEMBL4288647 1 -
CHEMBL1939444 1 -
CHEMBL4285306 1 -
CHEMBL4293122 1 -
CHEMBL4281873 1 -
CHEMBL4289736 1 -
CHEMBL4278411 1 -
CHEMBL4286321 1 -
CHEMBL4281971 1 -
CHEMBL4291145 1 -
CHEMBL4277049 1 -
CHEMBL4291222 1 -
CHEMBL4285955 1 -
CHEMBL4287446 1 -
CHEMBL4290703 1 -
CHEMBL4279362 1 -
CHEMBL4287292 1 -
CHEMBL4283929 1 -
CHEMBL4291102 1 -
CHEMBL4276795 1 -
CHEMBL4280478 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4288744 IC50 = 2900.0 nM 5.54
CHEMBL4280516 IC50 = 7400.0 nM 5.13
CHEMBL4282817 IC50 = 9100.0 nM 5.04
CHEMBL4292242 IC50 = 9500.0 nM 5.02
CHEMBL4279400 IC50 = 13400.0 nM 4.87
CHEMBL4294511 IC50 = 15100.0 nM 4.82
CHEMBL4280931 IC50 = 17800.0 nM 4.75
CHEMBL4285399 IC50 = 18200.0 nM 4.74
CHEMBL4287324 IC50 = 23700.0 nM 4.62
CHEMBL4278506 IC50 - -
CHEMBL4289164 IC50 - -
CHEMBL4280855 IC50 - -
CHEMBL4277444 IC50 - -
CHEMBL4287737 IC50 - -
CHEMBL4294110 IC50 - -
CHEMBL4284336 IC50 - -
CHEMBL4288832 IC50 - -
CHEMBL4287031 IC50 - -
CHEMBL4291145 IC50 - -
CHEMBL4292578 IC50 - -
CHEMBL4279102 IC50 - -
CHEMBL4291075 IC50 - -
CHEMBL4280445 IC50 - -
CHEMBL4290444 IC50 - -
CHEMBL4282571 IC50 - -
CHEMBL4293848 IC50 - -
CHEMBL4277091 IC50 - -
CHEMBL1939442 IC50 - -
CHEMBL4294257 IC50 - -
CHEMBL4291222 IC50 - -
CHEMBL4280478 IC50 - -
CHEMBL4276795 IC50 - -
CHEMBL4291102 IC50 - -
CHEMBL4283929 IC50 - -
CHEMBL4287292 IC50 - -
CHEMBL4279362 IC50 - -
CHEMBL4290703 IC50 - -
CHEMBL4287446 IC50 - -
CHEMBL4285955 IC50 - -
CHEMBL4281971 IC50 - -
CHEMBL4277049 IC50 - -
CHEMBL4288647 IC50 - -
CHEMBL1939444 IC50 - -
CHEMBL4285306 IC50 - -
CHEMBL4293122 IC50 - -
CHEMBL4281873 IC50 - -
CHEMBL4289736 IC50 - -
CHEMBL4278411 IC50 - -
CHEMBL4286321 IC50 - -