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Assay Detail

CHEMBL4376265

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

Binding
Binding affinity to full length Mycobacterium tuberculosis tRNA (guanine(37)-N1)-methyltransferase expressed in Escherichia coli BL21 (DE3) by surface plasmon resonance assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mycobacterium tuberculosis
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

tRNA (guanine-N(1)-)-methyltransferase (CHEMBL4523933)
Type SINGLE PROTEIN
Organism Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)

Publication

Thienopyrimidinone Derivatives That Inhibit Bacterial tRNA (Guanine37-<i>N</i><sup>1</sup>)-Methyltransferase (TrmD) by Restructuring the Active Site with a Tyrosine-Flipping Mechanism.
Zhong W, Pasunooti KK, Balamkundu S, Wong YH, Nah Q, Gadi V, Gnanakalai S, Chionh YH, McBee ME, Gopal P, Lim SH, Olivier N, Buurman ET, Dick T, Liu CF, Lescar J, Dedon PC.
J Med Chem (2019) 62 : 7788 -7805
PubMed 31442049 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 5.57 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4517402 1 6.72
CHEMBL418052 S-ADENOSYLHOMOCYSTEINE 1 5.00
CHEMBL2431997 1 4.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4517402 Kd = 190.0 nM 6.72
CHEMBL418052 S-ADENOSYLHOMOCYSTEINE Kd = 10100.0 nM 5.00
CHEMBL2431997 Kd = 10400.0 nM 4.98