Reaction Details |
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Target | Prolyl endopeptidase FAP |
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Ligand | BDBM50134186 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1537821 (CHEMBL3737792) |
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IC50 | 22000±n/a nM |
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Citation | Chen, P; Feng, D; Qian, X; Apgar, J; Wilkening, R; Kuethe, JT; Gao, YD; Scapin, G; Cox, J; Doss, G; Eiermann, G; He, H; Li, X; Lyons, KA; Metzger, J; Petrov, A; Wu, JK; Xu, S; Weber, AE; Yan, Y; Roy, RS; Biftu, T Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. Bioorg Med Chem Lett25:5767-71 (2015) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Prolyl endopeptidase FAP |
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Name: | Prolyl endopeptidase FAP |
Synonyms: | APCE | Antiplasmin-cleaving enzyme FAP, soluble form | Dipeptidyl peptidase FAP | FAP | FAPalpha | Fibroblast activation protein alpha | Gelatine degradation protease FAP | Integral membrane serine protease | Post-proline cleaving enzyme | Prolyl endopeptidase FAP | SEPR_BOVIN | SIMP | Seprase | Serine integral membrane protease | Surface-expressed protease | Z-Pro-prolinal insensitive peptidase | ZIP |
Type: | PROTEIN |
Mol. Mass.: | 87742.67 |
Organism: | Bos taurus |
Description: | ChEMBL_116681 |
Residue: | 760 |
Sequence: | MKTWLKIVFGVATSAVLALLVMCIVLRPSRVHNSEESTTRALTLKDILNGTFSYKTFFPN
WISGQEYLHQSTDNNVVFYNIETGESYTILSNTTMKSVNASNYGLSPDRQFAYLESDYSK
LWRYSYTATYHIYDLTNGEFIRRNELPRPIQYLCWSPVGSKLAYVYQNNIYLKQRPEDPP
FQITYNGKENKIFNGIPDWVYEEEMLATKYALWWSPNGKFLAYAEFNDTEIPVIAYSYYG
DEQYPRTINIPYPKAGAKNPVVRIFIIDATYPEHIGPREVPVPAMIASSDYYFSWLTWVT
DDRICLQWLKRIQNVSVLSTCDFREDWQTWNCPKTQEHIEESRTGWAGGFFVSTPVFSHD
TISYYKIFSDKDGYKHIHYIRDTVENAIQITSGKWEAINIFRVTQDSLFYSSNEFEGYPG
RRNIYRISIGSHSPSKKCITCHLRKKRCQYYTASFSDYAKYYALVCYGPGLPISTLHDGR
TDQEIKILEDNKELENALKNIQLPKEEIKKLKVDDITLWYKMILPPQFDKSKKYPLLIQV
YGGPCSQSVRSIFAVSWISYLASKEGIVIALVDGRGTAFQGDKLLYAVYRKLGVYEVEDQ
ITAVRKFIEMGFIDEKRIAIWGWSYGGYVSSLALASGTGLFKCGIAVAPVSSWEYYASIY
TERFMGLPTKDDNLKHYKNSTVMARAEYFRNVDYLLIHGTADDNVHFQNSAQIAKALVNA
QVDFQAMWYSDQNHGLSGLSTKHLYTHMTHFLKQCFSLSD
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BDBM50134186 |
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n/a |
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Name | BDBM50134186 |
Synonyms: | CHEMBL3734964 |
Type | Small organic molecule |
Emp. Form. | C20H23F2N5O2 |
Mol. Mass. | 403.4257 |
SMILES | N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1Cc2[nH]nc(NC(=O)C3CC3)c2C1 |r| |
Structure |
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