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Assay Detail

CHEMBL3579429

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Binding
Inhibition of N-terminal hexa-histidine tagged Mycobacterium tuberculosis HGPRT expressed in Escherichia coli BL-21(DE3) using PRib-PP substrate and guanine
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mycobacterium tuberculosis
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

First Crystal Structures of Mycobacterium tuberculosis 6-Oxopurine Phosphoribosyltransferase: Complexes with GMP and Pyrophosphate and with Acyclic Nucleoside Phosphonates Whose Prodrugs Have Antituberculosis Activity.
Eng WS, Hocková D, Špaček P, Janeba Z, West NP, Woods K, Naesens LM, Keough DT, Guddat LW.
J Med Chem (2015) 58 : 4822 -4838
PubMed 25915781 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 5.45 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2325754 1 6.16
CHEMBL2325752 1 6.11
CHEMBL3578115 1 5.95
CHEMBL3394316 1 5.85
CHEMBL3578110 1 5.80
CHEMBL3578114 1 5.80
CHEMBL1229838 1 5.75
CHEMBL2325753 1 5.11
CHEMBL3578112 1 4.80
CHEMBL1233207 1 4.75
CHEMBL3578111 1 4.65
CHEMBL3578113 1 4.64
CHEMBL3578109 1 -
CHEMBL3394313 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2325754 Ki = 690.0 nM 6.16
CHEMBL2325752 Ki = 770.0 nM 6.11
CHEMBL3578115 Ki = 1130.0 nM 5.95
CHEMBL3394316 Ki = 1400.0 nM 5.85
CHEMBL3578110 Ki = 1600.0 nM 5.80
CHEMBL3578114 Ki = 1600.0 nM 5.80
CHEMBL1229838 Ki = 1760.0 nM 5.75
CHEMBL2325753 Ki = 7700.0 nM 5.11
CHEMBL3578112 Ki = 15900.0 nM 4.80
CHEMBL1233207 Ki = 18000.0 nM 4.75
CHEMBL3578111 Ki = 22500.0 nM 4.65
CHEMBL3578113 Ki = 22700.0 nM 4.64
CHEMBL3578109 Ki > 50000.0 nM -
CHEMBL3394313 Ki > 50000.0 nM -