Target family: CYP3 family (type: enzyme)
Target: CYP3A4

Ligand: AMG-337 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.300000190734863 pIC50
Reference (Journal): Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: azalanstat (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.550000190734863 pKi
Reference (Journal): Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering.
Published in: J Med Chem

Ligand: BMS-536924 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pIC50
Reference (Journal): Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.
Published in: J Med Chem

Ligand: compound 1a [PMID: 18573659] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.71999979019165 pIC50
Reference (Journal): Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides.
Published in: Bioorg Med Chem Lett

Ligand: efavirenz (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1998), EMA (1999)
Primary target: no
Median affinity: 4.760000228881836 pIC50
Reference (Journal): Inhibition of human cytochrome P450 isoforms by nonnucleoside reverse transcriptase inhibitors.
Published in: J Clin Pharmacol

Ligand: ketoconazole (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1981), EMA (2014)
Primary target: no
Median affinity: 7 pKi
Reference (Journal): Ritonavir is the best alternative to ketoconazole as an index inhibitor of cytochrome P450-3A in drug-drug interaction studies.
Published in: Br J Clin Pharmacol

Ligand: nefazodone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1994)
Primary target: no
Median affinity: 6 pKi
Reference (Journal): Nefazodone, meta-chlorophenylpiperazine, and their metabolites in vitro: cytochromes mediating transformation, and P450-3A4 inhibitory actions.
Published in: Psychopharmacology (Berl.)

Ligand: nefazodone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1994)
Primary target: no
Median affinity: 6 pKi
Reference (Journal): Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks.
Published in: J Med Chem

Ligand: noscapine (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: ritonavir (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (1996)
Primary target: no
Median affinity: 7 pKi
Reference (Journal): Rapid clinical induction of hepatic cytochrome P4502B6 activity by ritonavir.
Published in: Antimicrob Agents Chemother

Ligand: troleandomycin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1969)
Primary target: no
Median affinity: 7.800000190734863 pKi
Reference (Journal): Current Approaches for Investigating and Predicting Cytochrome P450 3A4-Ligand Interactions.
Published in: Adv Exp Med Biol

Ligand: verapamil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity: 6.21999979019165 pKi
Reference (Journal): Inhibitory effects of verapamil and diltiazem on simvastatin metabolism in human liver microsomes.
Published in: Br J Clin Pharmacol

Ligand: voxelotor (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2019), EMA (2022)
Primary target: no
Median affinity: 4.900000095367432 pIC50
Reference (Journal): Discovery of GBT440, an Orally Bioavailable R-State Stabilizer of Sickle Cell Hemoglobin.
Published in: ACS Med Chem Lett