Reaction Details Report a problem with these data
Target
Cytochrome P450 2D6
Ligand
BDBM26471
Substrate
BDBM26482
Meas. Tech.
Homogeneous Time-Resolved Fluorescence (HTRF) Enzyme Assay
IC50
18000±n/a nM
Citation
Harris, PA; Boloor, A; Cheung, M; Kumar, R; Crosby, RM; Davis-Ward, RG; Epperly, AH; Hinkle, KW; Hunter, RN; Johnson, JH; Knick, VB; Laudeman, CP; Luttrell, DK; Mook, RA; Nolte, RT; Rudolph, SK; Szewczyk, JR; Truesdale, AT; Veal, JM; Wang, L; Stafford, JA Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor. J Med Chem 51:4632-40 (2008) [PubMed] Article
More Info.:
Target
Name:
Cytochrome P450 2D6
Synonyms:
CP2D6_HUMAN | CYP2D6 | CYP2DL1 | CYPIID6 | Cytochrome P450 2D6 (CYP2D6) | Debrisoquine 4-hydroxylase | P450-DB1
Type:
Protein
Mol. Mass.:
55774.82
Organism:
Homo sapiens (Human)
Description:
P10635
Residue:
497
Sequence:
MGLEALVPLAVIVAIFLLLVDLMHRRQRWAARYPPGPLPLPGLGNLLHVDFQNTPYCFDQLRRRFGDVFSLQLAWTPVVVLNGLAAVREALVTHGEDTADRPPVPITQILGFGPRSQGVFLARYGPAWREQRRFSVSTLRNLGLGKKSLEQWVTEEAACLCAAFANHSGRPFRPNGLLDKAVSNVIASLTCGRRFEYDDPRFLRLLDLAQEGLKEESGFLREVLNAVPVLLHIPALAGKVLRFQKAFLTQLDELLTEHRMTWDPAQPPRDLTEAFLAEMEKAKGNPESSFNDENLRIVVADLFSAGMVTTSTTLAWGLLLMILHPDVQRRVQQEIDDVIGQVRRPEMGDQAHMPYTTAVIHEVQRFGDIVPLGVTHMTSRDIEVQGFRIPKGTTLITNLSSVLKDEAVWEKPFRFHPEHFLDAQGHFVKPEAFLPFSAGRRACLGEPLARMELFLFFTSLLQHFSFSVPTGQPRPSHHGVFAFLVSPSPYELCAVPR
Inhibitor
Name:
BDBM26471
Synonyms:
3-({4-[methyl(2-methyl-2H-indazol-6-yl)amino]pyrimidin-2-yl}amino)benzene-1-sulfonamide | 3-aminobenzene sulfonamide, 12e
Type:
Small organic molecule
Emp. Form.:
C19H19N7O2S
Mol. Mass.:
409.465
SMILES:
CN(c1ccc2cn(C)nc2c1)c1ccnc(Nc2cccc(c2)S(N)(=O)=O)n1