Assay Detail

CHEMBL5517264

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ADMET

Inhibition of CYP2D6 (unknown origin) using dextro-methorphan as substrate

ChEMBL ↗

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Target

Cytochrome P450 2D6 (CHEMBL289) ↗

Open DB target context

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Cytochrome P450 2D6 (CHEMBL289) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Cytochrome P450 2D6

CHEMBL289

Anchored from Assay target.

Protein identity Cytochrome P450 2D6

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
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Cytochrome P450 2D6 (CHEMBL289) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of Clinical Candidate PF-06648671: A Potent γ-Secretase Modulator for the Treatment of Alzheimer's Disease.

Pettersson M, Johnson DS, Humphrey JM, Am Ende CW, Butler TW, Dorff PH, Efremov IV, Evrard E, Green ME, Helal CJ, Kauffman GW, Mullins PB, Navaratnam T, O'Donnell CJ, O'Sullivan TJ, Patel NC, Stepan AF, Stiff CM, Subramanyam C, Trapa P, Tran TP, Vetelino BC, Yang E, Xie L, Pustilnik LR, Steyn SJ, Wood KM, Bales KR, Hajos-Korcsok E, Verhoest PR.
J Med Chem (2024) 67 : 10248 -10262
PubMed 38848667 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	4.80	4.80

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3951810	—	—	1	4.80

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3951810	—	IC50	=	16000.0	nM	4.80