Reaction Details Report a problem with these data
Target
Coagulation factor X
Ligand
BDBM50231272
Substrate
n/a
Meas. Tech.
ChEMBL_460575 (CHEMBL926651)
Ki
15.9±n/a nM
Citation
Lee, YK; Parks, DJ; Lu, T; Thieu, TV; Markotan, T; Pan, W; McComsey, DF; Milkiewicz, KL; Crysler, CS; Ninan, N; Abad, MC; Giardino, EC; Maryanoff, BE; Damiano, BP; Player, MR 7-fluoroindazoles as potent and selective inhibitors of factor Xa. J Med Chem 51:282-97 (2008) [PubMed] Article
More Info.:
Target
Name:
Coagulation factor X
Synonyms:
Activated coagulation factor X (FXa) | Activated factor Xa heavy chain | Coagulation factor X precursor | Coagulation factor Xa | F10 | FA10_HUMAN | Factor X heavy chain | Factor X light chain | Factor Xa | Stuart factor | Stuart-Prower factor
Type:
Enzyme
Mol. Mass.:
54726.60
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
488
Sequence:
MGRPLHLVLLSASLAGLLLLGESLFIRREQANNILARVTRANSFLEEMKKGHLERECMEETCSYEEAREVFEDSDKTNEFWNKYKDGDQCETSPCQNQGKCKDGLGEYTCTCLEGFEGKNCELFTRKLCSLDNGDCDQFCHEEQNSVVCSCARGYTLADNGKACIPTGPYPCGKQTLERRKRSVAQATSSSGEAPDSITWKPYDAADLDPTENPFDLLDFNQTQPERGDNNLTRIVGGQECKDGECPWQALLINEENEGFCGGTILSEFYILTAAHCLYQAKRFKVRVGDRNTEQEEGGEAVHEVEVVIKHNRFTKETYDFDIAVLRLKTPITFRMNVAPACLPERDWAESTLMTQKTGIVSGFGRTHEKGRQSTRLKMLEVPYVDRNSCKLSSSFIITQNMFCAGYDTKQEDACQGDSGGPHVTRFKDTYFVTGIVSWGEGCARKGKYGIYTKVTAFLKWIDRSMKTRGLPKAKSHAPEVITSSPLK
Inhibitor
Name:
BDBM50231272
Synonyms:
1-(3-amino-1,2-benzisoxazol-5-yl)-6-(4-{2-[(dimethylamino)methyl]-1H-imidazol-1-yl}-2-fluorophenyl)-7-fluoro-1H-indazole-3-carboxamide | 1-(3-aminobenzo[d]isoxazol-5-yl)-6-[4-(2-dimethylaminomethylimidazol-1-yl)-2-fluorophenyl]-7-fluoro-1H-indazole-3-carboxylicacid amide | CHEMBL398870
Type:
Small organic molecule
Emp. Form.:
C27H22F2N8O2
Mol. Mass.:
528.5128
SMILES:
CN(C)Cc1nccn1-c1ccc(c(F)c1)-c1ccc2c(nn(-c3ccc4onc(N)c4c3)c2c1F)C(N)=O