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Assay Detail

CHEMBL934304

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

Binding
Inhibition of transketolase by TPPK/apo-TK coupled assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Transketolase (CHEMBL4983)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors.
Thomas AA, Le Huerou Y, De Meese J, Gunawardana I, Kaplan T, Romoff TT, Gonzales SS, Condroski K, Boyd SA, Ballard J, Bernat B, DeWolf W, Han M, Lee P, Lemieux C, Pedersen R, Pheneger J, Poch G, Smith D, Sullivan F, Weiler S, Wright SK, Lin J, Brandhuber B, Vigers G.
Bioorg Med Chem Lett (2008) 18 : 2206 -2210
PubMed 18267359 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 25 7.27 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL255603 1 8.15
CHEMBL256627 1 8.00
CHEMBL256831 1 7.64
CHEMBL402329 1 7.60
CHEMBL402566 1 7.60
CHEMBL255340 1 7.57
CHEMBL258077 1 7.55
CHEMBL256454 1 7.54
CHEMBL252086 1 7.48
CHEMBL271044 1 7.47
CHEMBL270632 1 7.44
CHEMBL403365 1 7.44
CHEMBL255541 1 7.40
CHEMBL270613 1 7.34
CHEMBL255542 1 7.28
CHEMBL429246 1 7.24
CHEMBL271521 1 7.19
CHEMBL403212 1 7.12
CHEMBL270168 1 6.98
CHEMBL270384 1 6.96
CHEMBL255339 1 6.92
CHEMBL402065 1 6.85
CHEMBL256267 1 6.66
CHEMBL257929 1 6.51
CHEMBL270385 1 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL255603 Kd = 7.0 nM 8.15
CHEMBL256627 Kd = 10.0 nM 8.00
CHEMBL256831 Kd = 23.0 nM 7.64
CHEMBL402329 Kd = 25.0 nM 7.60
CHEMBL402566 Kd = 25.0 nM 7.60
CHEMBL255340 Kd = 27.0 nM 7.57
CHEMBL258077 Kd = 28.0 nM 7.55
CHEMBL256454 Kd = 29.0 nM 7.54
CHEMBL252086 Kd = 33.0 nM 7.48
CHEMBL271044 Kd = 34.0 nM 7.47
CHEMBL270632 Kd = 36.0 nM 7.44
CHEMBL403365 Kd = 36.0 nM 7.44
CHEMBL255541 Kd = 40.0 nM 7.40
CHEMBL270613 Kd = 46.0 nM 7.34
CHEMBL255542 Kd = 53.0 nM 7.28
CHEMBL429246 Kd = 57.0 nM 7.24
CHEMBL271521 Kd = 64.0 nM 7.19
CHEMBL403212 Kd = 75.0 nM 7.12
CHEMBL270168 Kd = 104.0 nM 6.98
CHEMBL270384 Kd = 109.0 nM 6.96
CHEMBL255339 Kd = 120.0 nM 6.92
CHEMBL402065 Kd = 140.0 nM 6.85
CHEMBL256267 Kd = 220.0 nM 6.66
CHEMBL257929 Kd = 310.0 nM 6.51
CHEMBL270385 Kd = 1460.0 nM 5.84