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Assay Detail

CHEMBL972645

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

Binding
Inhibition of luciferin binding site of Photuris pennsylvanica luciferase by competitive inhibition assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Photuris pennsylvanica
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Luciferin 4-monooxygenase (CHEMBL5150)
Type SINGLE PROTEIN
Organism Photuris pennsylvanica

Publication

A basis for reduced chemical library inhibition of firefly luciferase obtained from directed evolution.
Auld DS, Zhang YQ, Southall NT, Rai G, Landsman M, MacLure J, Langevin D, Thomas CJ, Austin CP, Inglese J.
J Med Chem (2009) 52 : 1450 -1458
PubMed 19215089 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.62 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL92816 1 6.50
CHEMBL460508 1 6.44
CHEMBL508666 1 6.30
CHEMBL460507 1 6.17
CHEMBL490083 1 6.07
CHEMBL507630 1 5.96
CHEMBL449008 1 5.85
CHEMBL462620 1 5.72
CHEMBL201610 1 5.72
CHEMBL462617 1 5.68
CHEMBL328430 1 5.57
CHEMBL129236 1 5.51
CHEMBL453117 1 5.42
CHEMBL460500 1 5.42
CHEMBL511869 1 5.39
CHEMBL460501 1 5.37
CHEMBL453116 1 5.31
CHEMBL452608 1 5.25
CHEMBL512398 1 5.21
CHEMBL499212 1 5.11
CHEMBL506342 1 5.11
CHEMBL462613 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL92816 IC50 = 320.0 nM 6.50
CHEMBL460508 IC50 = 360.0 nM 6.44
CHEMBL508666 IC50 = 500.0 nM 6.30
CHEMBL460507 IC50 = 670.0 nM 6.17
CHEMBL490083 IC50 = 860.0 nM 6.07
CHEMBL507630 IC50 = 1100.0 nM 5.96
CHEMBL449008 IC50 = 1400.0 nM 5.85
CHEMBL462620 IC50 = 1900.0 nM 5.72
CHEMBL201610 IC50 = 1900.0 nM 5.72
CHEMBL462617 IC50 = 2100.0 nM 5.68
CHEMBL328430 IC50 = 2700.0 nM 5.57
CHEMBL129236 IC50 = 3100.0 nM 5.51
CHEMBL453117 IC50 = 3800.0 nM 5.42
CHEMBL460500 IC50 = 3800.0 nM 5.42
CHEMBL511869 IC50 = 4100.0 nM 5.39
CHEMBL460501 IC50 = 4300.0 nM 5.37
CHEMBL453116 IC50 = 4900.0 nM 5.31
CHEMBL452608 IC50 = 5600.0 nM 5.25
CHEMBL512398 IC50 = 6100.0 nM 5.21
CHEMBL499212 IC50 = 7700.0 nM 5.11
CHEMBL506342 IC50 = 7800.0 nM 5.11
CHEMBL462613 IC50 = 30000.0 nM 4.52