Assay Detail

CHEMBL4827366

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ADMET

Reversible inhibition of CYP3A4 in human liver microsomes at 10 uM using midazolam as substrate preincubated for 10 mins followed by NADPH addition by LC/MS/MS analysis

ChEMBL ↗

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Target

Cytochrome P450 3A4 (CHEMBL340) ↗

Open DB target context

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Cytochrome P450 3A4 (CHEMBL340) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Cytochrome P450 3A4

CHEMBL340

Anchored from Assay target.

Protein identity Cytochrome P450 3A4

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
Tissue	Liver
Subcellular	Microsomes
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Cytochrome P450 3A4 (CHEMBL340) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer.

Liang J, Zbieg JR, Blake RA, Chang JH, Daly S, DiPasquale AG, Friedman LS, Gelzleichter T, Gill M, Giltnane JM, Goodacre S, Guan J, Hartman SJ, Ingalla ER, Kategaya L, Kiefer JR, Kleinheinz T, Labadie SS, Lai T, Li J, Liao J, Liu Z, Mody V, McLean N, Metcalfe C, Nannini MA, Oeh J, O'Rourke MG, Ortwine DF, Ran Y, Ray NC, Roussel F, Sambrone A, Sampath D, Schutt LK, Vinogradova M, Wai J, Wang T, Wertz IE, White JR, Yeap SK, Young A, Zhang B, Zheng X, Zhou W, Zhong Y, Wang X.
J Med Chem (2021) 64 : 11841 -11856
PubMed 34251202 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	5.38	5.57

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4866043	—	—	1	5.57
CHEMBL4650316	GIREDESTRANT	3.0	1	5.19

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4866043	—	IC50	=	2700.0	nM	5.57
CHEMBL4650316	GIREDESTRANT	IC50	=	6500.0	nM	5.19