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Assay Detail

CHEMBL4413429

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

ADMET
Inhibition of human CYP1A2 in presence of NADPH by luciferase reporter gene assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytochrome P450 1A2 (CHEMBL3356)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, Synthesis, and Biological Evaluation of New 1-(Aryl-1 H-pyrrolyl)(phenyl)methyl-1 H-imidazole Derivatives as Antiprotozoal Agents.
Saccoliti F, Madia VN, Tudino V, De Leo A, Pescatori L, Messore A, De Vita D, Scipione L, Brun R, Kaiser M, Mäser P, Calvet CM, Jennings GK, Podust LM, Pepe G, Cirilli R, Faggi C, Di Marco A, Battista MR, Summa V, Costi R, Di Santo R.
J Med Chem (2019) 62 : 1330 -1347
PubMed 30615444 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.76 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4468270 1 6.40
CHEMBL4551139 1 5.92
CHEMBL4569370 1 5.70
CHEMBL405845 FURAFYLLINE 2.0 1 5.64
CHEMBL315874 1 5.16
CHEMBL4438726 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4468270 IC50 = 400.0 nM 6.40
CHEMBL4551139 IC50 = 1200.0 nM 5.92
CHEMBL4569370 IC50 = 2000.0 nM 5.70
CHEMBL405845 FURAFYLLINE IC50 = 2300.0 nM 5.64
CHEMBL315874 IC50 = 7000.0 nM 5.16
CHEMBL4438726 IC50 > 30000.0 nM -