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Target
Cytochrome P450 3A4
Ligand
BDBM50572808
Substrate
n/a
Meas. Tech.
ChEMBL_2118300 (CHEMBL4827366)
IC50
6500±n/a nM
Citation
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 GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer. J Med Chem 64:11841-11856 (2021) [PubMed] Article
More Info.:
Target
Name:
Cytochrome P450 3A4
Synonyms:
Albendazole monooxygenase | Albendazole sulfoxidase | CP3A4_HUMAN | CYP3A3 | CYP3A4 | CYPIIIA3 | CYPIIIA4 | Cytochrome P450 3A3 | Cytochrome P450 3A4 (CYP3A4) | Cytochrome P450 HLp | Nifedipine oxidase | Quinine 3-monooxygenase | Taurochenodeoxycholate 6-alpha-hydroxylase
Type:
Enzyme
Mol. Mass.:
57349.57
Organism:
Human
Description:
n/a
Residue:
503
Sequence:
MALIPDLAMETWLLLAVSLVLLYLYGTHSHGLFKKLGIPGPTPLPFLGNILSYHKGFCMFDMECHKKYGKVWGFYDGQQPVLAITDPDMIKTVLVKECYSVFTNRRPFGPVGFMKSAISIAEDEEWKRLRSLLSPTFTSGKLKEMVPIIAQYGDVLVRNLRREAETGKPVTLKDVFGAYSMDVITSTSFGVNIDSLNNPQDPFVENTKKLLRFDFLDPFFLSITVFPFLIPILEVLNICVFPREVTNFLRKSVKRMKESRLEDTQKHRVDFLQLMIDSQNSKETESHKALSDLELVAQSIIFIFAGYETTSSVLSFIMYELATHPDVQQKLQEEIDAVLPNKAPPTYDTVLQMEYLDMVVNETLRLFPIAMRLERVCKKDVEINGMFIPKGVVVMIPSYALHRDPKYWTEPEKFLPERFSKKNKDNIDPYIYTPFGSGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLSLGGLLQPEKPVVLKVESRDGTVSGA