Reaction Details Report a problem with these data
Target
Urokinase-type plasminogen activator
Ligand
BDBM50301987
Substrate
n/a
Meas. Tech.
ChEMBL_599341 (CHEMBL1042862)
IC50
130±n/a nM
Citation
West, CW; Adler, M; Arnaiz, D; Chen, D; Chu, K; Gualtieri, G; Ho, E; Huwe, C; Light, D; Phillips, G; Pulk, R; Sukovich, D; Whitlow, M; Yuan, S; Bryant, J Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA). Bioorg Med Chem Lett 19:5712-5 (2009) [PubMed] Article
More Info.:
Target
Name:
Urokinase-type plasminogen activator
Synonyms:
PLAU | U-plasminogen activator | UROK_HUMAN | Urokinase | Urokinase-type plasminogen activator (uPA) | Urokinase-type plasminogen activator/surface receptor
Type:
Enzyme
Mol. Mass.:
48528.62
Organism:
Homo sapiens (Human)
Description:
P00749
Residue:
431
Sequence:
MRALLARLLLCVLVVSDSKGSNELHQVPSNCDCLNGGTCVSNKYFSNIHWCNCPKKFGGQHCEIDKSKTCYEGNGHFYRGKASTDTMGRPCLPWNSATVLQQTYHAHRSDALQLGLGKHNYCRNPDNRRRPWCYVQVGLKPLVQECMVHDCADGKKPSSPPEELKFQCGQKTLRPRFKIIGGEFTTIENQPWFAAIYRRHRGGSVTYVCGGSLISPCWVISATHCFIDYPKKEDYIVYLGRSRLNSNTQGEMKFEVENLILHKDYSADTLAHHNDIALLKIRSKEGRCAQPSRTIQTICLPSMYNDPQFGTSCEITGFGKENSTDYLYPEQLKMTVVKLISHRECQQPHYYGSEVTTKMLCAADPQWKTDSCQGDSGGPLVCSLQGRMTLTGIVSWGRGCALKDKPGVYTRVSHFLPWIRSHTKEENGLAL
Inhibitor
Name:
BDBM50301987
Synonyms:
2-(6-(3'-(aminomethyl)biphenyl-3-yloxy)-3,5-difluoro-4-(methylamino)pyridin-2-yloxy)-4-(dimethylamino)benzoic acid | CHEMBL569560
Type:
Small organic molecule
Emp. Form.:
C28H26F2N4O4
Mol. Mass.:
520.5272
SMILES:
CNc1c(F)c(Oc2cccc(c2)-c2cccc(CN)c2)nc(Oc2cc(ccc2C(O)=O)N(C)C)c1F