Reaction Details Report a problem with these data
Target
Coagulation factor X
Ligand
BDBM639340
Substrate
n/a
Meas. Tech.
Enzymatic Activity Assay
IC50
0.450±n/a nM
Citation
Beck, H; Mesch, S; Vakalopoulos, A; Pfaff, N; Zimmermann, S; Follmann, M; Kersten, E; Levilain, G; Partikel, K; Broehl, AP; Heitmeier, S; Dietze-Torres, J; Lehmann, L; Gericke, KM; Süßmeier, F; Bärfacker, L; Hillisch, A; Tersteegen, A; Buchmüller, A; Gerdes, C SUBSTITUTED S-ALANINATE DERIVATIVES US Patent US20230391761 Publication Date 12/7/2023
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:
BDBM639340
Synonyms:
2-(1-Methyl-1H-imidazol-2-yl)ethyl 3-{[(5-chloro-2-thienyl)carbonyl]amino}-N-{[2-methyl-3-(2-oxopyrrolidin-1-yl)phenyl]sulfonyl}-S-alaninate | US20230391761, Reference 8
Type:
Small organic molecule
Emp. Form.:
C25H28ClN5O6S2
Mol. Mass.:
594.103
SMILES:
Cc1c(cccc1S(=O)(=O)N[C@@H](CNC(=O)c1ccc(Cl)s1)C(=O)OCCc1nccn1C)N1CCCC1=O |r|