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Assay Detail

CHEMBL1805489

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

Binding
Inhibition of human QR2 expressed in Escherichia coli BL21 (DE3) using MTT and NMeH as substrate assessed as formazan formation
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Ribosyldihydronicotinamide dehydrogenase [quinone] (CHEMBL3959)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potential chemopreventive agents based on the structure of the lead compound 2-bromo-1-hydroxyphenazine, isolated from Streptomyces species, strain CNS284.
Conda-Sheridan M, Marler L, Park EJ, Kondratyuk TP, Jermihov K, Mesecar AD, Pezzuto JM, Asolkar RN, Fenical W, Cushman M.
J Med Chem (2010) 53 : 8688 -8699
PubMed 21105712 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 5.32 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1802205 1 6.80
CHEMBL1802199 1 6.73
CHEMBL1802264 1 6.50
CHEMBL1802260 1 6.35
CHEMBL1802271 1 6.32
CHEMBL1802203 1 6.16
CHEMBL1802258 1 5.85
CHEMBL1802277 1 5.54
CHEMBL1802261 1 5.48
CHEMBL1802272 1 5.46
CHEMBL1802270 1 5.39
CHEMBL1802267 1 5.32
CHEMBL1802266 1 4.98
CHEMBL1802269 1 4.95
CHEMBL1802273 BENZO[B]PHENAZINE 1 4.95
CHEMBL1379740 1 4.93
CHEMBL1802259 1 4.87
CHEMBL1420181 1 4.82
CHEMBL1802263 1 4.74
CHEMBL1802200 1 4.73
CHEMBL1802202 1 4.57
CHEMBL1802197 1 4.51
CHEMBL1802265 1 4.45
CHEMBL1802201 1 4.43
CHEMBL1802262 1 4.22
CHEMBL1802196 1 -
CHEMBL1802268 1 -
CHEMBL1802204 1 -
CHEMBL1802198 1 -
CHEMBL1802274 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1802205 IC50 = 160.0 nM 6.80
CHEMBL1802199 IC50 = 186.0 nM 6.73
CHEMBL1802264 IC50 = 320.0 nM 6.50
CHEMBL1802260 IC50 = 450.0 nM 6.35
CHEMBL1802271 IC50 = 480.0 nM 6.32
CHEMBL1802203 IC50 = 690.0 nM 6.16
CHEMBL1802258 IC50 = 1400.0 nM 5.85
CHEMBL1802277 IC50 = 2900.0 nM 5.54
CHEMBL1802261 IC50 = 3300.0 nM 5.48
CHEMBL1802272 IC50 = 3500.0 nM 5.46
CHEMBL1802270 IC50 = 4100.0 nM 5.39
CHEMBL1802267 IC50 = 4800.0 nM 5.32
CHEMBL1802266 IC50 = 10500.0 nM 4.98
CHEMBL1802269 IC50 = 11300.0 nM 4.95
CHEMBL1802273 BENZO[B]PHENAZINE IC50 = 11200.0 nM 4.95
CHEMBL1379740 IC50 = 11700.0 nM 4.93
CHEMBL1802259 IC50 = 13500.0 nM 4.87
CHEMBL1420181 IC50 = 15300.0 nM 4.82
CHEMBL1802263 IC50 = 18200.0 nM 4.74
CHEMBL1802200 IC50 = 18500.0 nM 4.73
CHEMBL1802202 IC50 = 26900.0 nM 4.57
CHEMBL1802197 IC50 = 31100.0 nM 4.51
CHEMBL1802265 IC50 = 35500.0 nM 4.45
CHEMBL1802201 IC50 = 36800.0 nM 4.43
CHEMBL1802262 IC50 = 60800.0 nM 4.22
CHEMBL1802196 IC50 - -
CHEMBL1802268 IC50 - -
CHEMBL1802204 IC50 - -
CHEMBL1802198 IC50 - -
CHEMBL1802274 IC50 - -
CHEMBL1802275 IC50 - -
CHEMBL1802276 IC50 - -