Assay Detail

CHEMBL4432027

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ADMET

Inhibition of human microsomal CYP1A2 expressed in baculovirus infected BTI-TN-5B1-4 cells incubated for 30 mins by luciferase assay

ChEMBL ↗

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Target

Cytochrome P450 1A2 (CHEMBL3356) ↗

Open DB target context

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Cytochrome P450 1A2 (CHEMBL3356) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Cytochrome P450 1A2

CHEMBL3356

Anchored from Assay target.

Protein identity Cytochrome P450 1A2

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	ADMET
Organism	Homo sapiens
Cell Type	BTI-TN-5B1-4
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Cytochrome P450 1A2 (CHEMBL3356) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Profiling of Flavonol Derivatives for the Development of Antitrypanosomatidic Drugs.

Borsari C, Luciani R, Pozzi C, Poehner I, Henrich S, Trande M, Cordeiro-da-Silva A, Santarem N, Baptista C, Tait A, Di Pisa F, Dello Iacono L, Landi G, Gul S, Wolf M, Kuzikov M, Ellinger B, Reinshagen J, Witt G, Gribbon P, Kohler M, Keminer O, Behrens B, Costantino L, Tejera Nevado P, Bifeld E, Eick J, Clos J, Torrado J, Jiménez-Antón MD, Corral MJ, Alunda JM, Pellati F, Wade RC, Ferrari S, Mangani S, Costi MP.
J Med Chem (2016) 59 : 7598 -7616
PubMed 27411733 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	5.21	5.21

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4464764	—	—	1	5.21

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4464764	—	IC50	=	6100.0	nM	5.21