Target
1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial
Ligand
BDBM8610
Substrate
n/a
Meas. Tech.
CYP24A1Inhibition Assay
Ki
32± 5 nM
Citation
 Zhu, JBarycki, RChiellini, GDeluca, HF Screening of selective inhibitors of 1a,25-dihydroxyvitamin D3 24-hydroxylase using recombinant human enzyme expressed in Escherichia coli. Biochemistry 49:10403-11 (2010) [PubMed]  Article 
Target
Name:
1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial
Synonyms:
1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial | CP24A_HUMAN | CYP24 | CYP24A1 | Cytochrome P450 24A1
Type:
Protein
Mol. Mass.:
58889.66
Organism:
Homo sapiens (Human)
Description:
Q07973
Residue:
514
Sequence:
MSSPISKSRSLAAFLQQLRSPRQPPRLVTSTAYTSPQPREVPVCPLTAGGETQNAAALPGPTSWPLLGSLLQILWKGGLKKQHDTLVEYHKKYGKIFRMKLGSFESVHLGSPCLLEALYRTESAYPQRLEIKPWKAYRDYRKEGYGLLILEGEDWQRVRSAFQKKLMKPGEVMKLDNKINEVLADFMGRIDELCDERGHVEDLYSELNKWSFESICLVLYEKRFGLLQKNAGDEAVNFIMAIKTMMSTFGRMMVTPVELHKSLNTKVWQDHTLAWDTIFKSVKACIDNRLEKYSQQPSADFLCDIYHQNRLSKKELYAAVTELQLAAVETTANSLMWILYNLSRNPQVQQKLLKEIQSVLPENQVPRAEDLRNMPYLKACLKESMRLTPSVPFTTRTLDKATVLGEYALPKGTVLMLNTQVLGSSEDNFEDSSQFRPERWLQEKEKINPFAHLPFGVGKRMCIGRRLAELQLHLALCWIVRKYDIQATDNEPVEMLHSGTLVPSRELPIAFCQR
  
Inhibitor
Name:
BDBM8610
Synonyms:
1-[4-(4-{[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]ethan-1-one | 24F2-1,25(OH)D3 | CHEMBL75 | KTZ | Ketoconazole | Ketoconazole (k) | US9138393, Ketoconozole | US9144538, Ketoconozole
Type:
Small organic molecule
Emp. Form.:
C26H28Cl2N4O4
Mol. Mass.:
531.431
SMILES:
[H][C@]1(COc2ccc(cc2)N2CCN(CC2)C(C)=O)CO[C@@](Cn2ccnc2)(O1)c1ccc(Cl)cc1Cl |r|
Structure:
Search PDB for entries with ligand similarity: