ARI-4175

pan-DPP inhibitor: IC50 0.0016 microM Dipeptidyl peptidase 4 (human); 0.0019 microM Dipeptidyl peptidase 9 (human); 0.0051 microM Dipeptidyl peptidase 8 (human)

General

Type : Boron compound, Peptide, Pyrrolidine

Chemical_Nomenclature : [(2R)-1-[(2S)-2-amino-3,3-dimethylbutanoyl]pyrrolidin-2-yl]boronic acid

Canonical SMILES : B([C@@H]1CCCN1C(=O)[C@H](C(C)(C)C)N)(O)O

InChI : InChI=1S\/C10H21BN2O3\/c1-10(2,3)8(12)9(14)13-6-4-5-7(13)11(15)16\/h7-8,15-16H,4-6,12H2,1-3H3\/t7-,8+\/m0\/s1

InChIKey : YLQGXGBOYJWXBT-JGVFFNPUSA-N

Other name(s) : Tle-boroPro  ||  CHEMBL63406  ||  BDBM50050520


MW : 228.1

Formula : C10H21BN2O3

CAS_number :

PubChem : 10704521

UniChem : YLQGXGBOYJWXBT-JGVFFNPUSA-N

Target

Families : ARI-4175 ligand of proteins in family
DPP4N_Peptidase_S9

References (6)

Title : A high-throughput, multiplexed assay for superfamily-wide profiling of enzyme activity - Bachovchin_2014_Nat.Chem.Biol_10_656
Author(s) : Bachovchin DA , Koblan LW , Wu W , Liu Y , Li Y , Zhao P , Woznica I , Shu Y , Lai JH , Poplawski SE , Kiritsy CP , Healey SE , DiMare M , Sanford DG , Munford RS , Bachovchin WW , Golub TR
Ref : Nat Chemical Biology , 10 :656 , 2014
Abstract :
PubMedSearch : Bachovchin_2014_Nat.Chem.Biol_10_656
PubMedID: 24997602
Gene_locus related to this paper: human-PPME1

Title : A high-throughput, multiplexed assay for superfamily-wide profiling of enzyme activity - Bachovchin_2014_Nat.Chem.Biol_10_656
Author(s) : Bachovchin DA , Koblan LW , Wu W , Liu Y , Li Y , Zhao P , Woznica I , Shu Y , Lai JH , Poplawski SE , Kiritsy CP , Healey SE , DiMare M , Sanford DG , Munford RS , Bachovchin WW , Golub TR
Ref : Nat Chemical Biology , 10 :656 , 2014
Abstract :
PubMedSearch : Bachovchin_2014_Nat.Chem.Biol_10_656
PubMedID: 24997602
Gene_locus related to this paper: human-PPME1

Title : A high-throughput, multiplexed assay for superfamily-wide profiling of enzyme activity - Bachovchin_2014_Nat.Chem.Biol_10_656
Author(s) : Bachovchin DA , Koblan LW , Wu W , Liu Y , Li Y , Zhao P , Woznica I , Shu Y , Lai JH , Poplawski SE , Kiritsy CP , Healey SE , DiMare M , Sanford DG , Munford RS , Bachovchin WW , Golub TR
Ref : Nat Chemical Biology , 10 :656 , 2014
Abstract :
PubMedSearch : Bachovchin_2014_Nat.Chem.Biol_10_656
PubMedID: 24997602
Gene_locus related to this paper: human-PPME1

Title : Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides - Coutts_1996_J.Med.Chem_39_2087
Author(s) : Coutts SJ , Kelly TA , Snow RJ , Kennedy CA , Barton RW , Adams J , Krolikowski DA , Freeman DM , Campbell SJ , Ksiazek JF , Bachovchin WW
Ref : Journal of Medicinal Chemistry , 39 :2087 , 1996
Abstract :
PubMedSearch : Coutts_1996_J.Med.Chem_39_2087
PubMedID: 8642568

Title : Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides - Coutts_1996_J.Med.Chem_39_2087
Author(s) : Coutts SJ , Kelly TA , Snow RJ , Kennedy CA , Barton RW , Adams J , Krolikowski DA , Freeman DM , Campbell SJ , Ksiazek JF , Bachovchin WW
Ref : Journal of Medicinal Chemistry , 39 :2087 , 1996
Abstract :
PubMedSearch : Coutts_1996_J.Med.Chem_39_2087
PubMedID: 8642568

Title : Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides - Coutts_1996_J.Med.Chem_39_2087
Author(s) : Coutts SJ , Kelly TA , Snow RJ , Kennedy CA , Barton RW , Adams J , Krolikowski DA , Freeman DM , Campbell SJ , Ksiazek JF , Bachovchin WW
Ref : Journal of Medicinal Chemistry , 39 :2087 , 1996
Abstract :
PubMedSearch : Coutts_1996_J.Med.Chem_39_2087
PubMedID: 8642568