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Target
Urokinase-type plasminogen activator
Ligand
BDBM50301982
Substrate
n/a
Meas. Tech.
ChEMBL_599341 (CHEMBL1042862)
IC50
25±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 
Target
Name:
Urokinase-type plasminogen activator
Synonyms:
3.4.21.73 | PLAU | U-plasminogen activator | UROK_HUMAN | Urokinase | Urokinase-type plasminogen activator (uPA) | Urokinase-type plasminogen activator chain B | Urokinase-type plasminogen activator long chain A | Urokinase-type plasminogen activator short chain A | Urokinase-type plasminogen activator/surface receptor | uPA
Type:
Enzyme
Mol. Mass.:
48528.62
Organism:
Homo sapiens (Human)
Description:
P00749
Residue:
431
Sequence:
MRALLARLLLCVLVVSDSKGSNELHQVPSNCDCLNGGTCVSNKYFSNIHWCNCPKKFGGQHCEIDKSKTCYEGNGHFYRGKASTDTMGRPCLPWNSATVLQQTYHAHRSDALQLGLGKHNYCRNPDNRRRPWCYVQVGLKLLVQECMVHDCADGKKPSSPPEELKFQCGQKTLRPRFKIIGGEFTTIENQPWFAAIYRRHRGGSVTYVCGGSLISPCWVISATHCFIDYPKKEDYIVYLGRSRLNSNTQGEMKFEVENLILHKDYSADTLAHHNDIALLKIRSKEGRCAQPSRTIQTICLPSMYNDPQFGTSCEITGFGKENSTDYLYPEQLKMTVVKLISHRECQQPHYYGSEVTTKMLCAADPQWKTDSCQGDSGGPLVCSLQGRMTLTGIVSWGRGCALKDKPGVYTRVSHFLPWIRSHTKEENGLAL
  
Inhibitor
Name:
BDBM50301982
Synonyms:
2-(6-(3'-(aminomethyl)biphenyl-3-yloxy)-4-(3-(dimethylamino)pyrrolidin-1-yl)-3,5-difluoropyridin-2-yloxy)-4-(dimethylamino)benzoic acid | CHEMBL572191
Type:
Small organic molecule
Emp. Form.:
C33H35F2N5O4
Mol. Mass.:
603.6589
SMILES:
CN(C)C1CCN(C1)c1c(F)c(Oc2cccc(c2)-c2cccc(CN)c2)nc(Oc2cc(ccc2C(O)=O)N(C)C)c1F
Structure:
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