Discovery and Characterization of Biased Allosteric Agonists of the Chemokine Receptor CXCR3

Journal of Medicinal Chemistry

Volumn 59, Issue 5, 2016, Pages 2222-2243

  Milanos, Lampros ^a   Brox, Regine ^a   Frank, Theresa ^a   Poklukar, Gašper ^a,b   Palmisano, Ralf ^a   Waibel, Reiner ^a   Einsiedel, Jürgen ^a   Dürr, Maximilian ^a   Ivanović Burmazović, Ivana ^a   Larsen, Olav ^c   Hjortø, Gertrud Malene ^c   Rosenkilde, Mette Marie ^c   Tschammer, Nuska ^a,d  

^a UNIVERSITY OF ERLANGEN NUREMBERG   (Germany)

^b UNIVERSITY OF LJUBLJANA   (Slovenia)

^c UNIVERSITY OF COPENHAGEN   (Denmark)

^d NanoTemper Technologies GmbH   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

2 [(BENZYLOXY)CARBONYL] 1,2,3,4 TETRAHYDROISOQUINOLINE 3 CARBOXYLIC ACID; 4 (4 METHYLPIPERAZIN 1 YL) 4 OXOBUTANOIC ACID; 4 (FURAN 2 YL) 4 OXOBUTANOIC ACID; 4 MORPHOLINO 4 OXOBUTANOIC ACID; 4 OXO 4 (PIPERIDIN 1 YL)BUTANOIC ACID; 4 OXO 4 (THIOPHEN 2 YL)BUTANOIC ACID; 4 [4 [ 3 [[ 5 [(TERT BUTOXYCARBONYL)AMINO] 6 [(2,2 DIPHENYLETHYL)AMINO] 6 OXOHEXYL]CARBAMOYL] 3,4 DIHYDROISOQUINOLIN 2(1H) 4 OXOBUTANOYL] 1 METHYLPIPERAZIN 1 IUM 2,2,2 TRIFLUOROACETATE; 6 [(2,2 DIPHENYLETHYL)AMINO] 6 OXO 5 [ 2 (4 OXO 4 PHENYLBUTANOYL) 1,2,3,4 TETRAHYDROISOQUINOLINE 3 CARBOXAMIDO]HEXAN 1 AMINIUM 2,2,2 TRIFLUOROACETATE; AMIDE; BENZYL 3 [[ 5 [(TERT BUTOXYCARBONYL)AMINO] 6 [(2,2 DIPHENYLETHYL)AMINO] 6 OXOHEXYL]CARBAMOYL] 3,4 DIHYDROISOQUINOLINE 2(1H)CARBOXYLATE; BENZYL TERT BUTYL [6 [(2,2 DIPHENYLETHYL)AMINO] 6 OXOHEXANE 1,5 DIYL]DICARBAMATE; BETA ARRESTIN 2; CHEMOKINE RECEPTOR AGONIST; CHEMOKINE RECEPTOR CXCR3 AGONIST; TERT BUTYL [ 1 [(2,2 DIPHENYLETHYL)AMINO] 1 OXO 6 [ 1,2,3,4 TETRAHYDROISOQUINOLINE 3 CARBOXAMIDO]HEXAN 2 YL]CARBAMATE; TERT BUTYL [ 1 [(2,2 DIPHENYLETHYL)AMINO] 1 OXO 6 [ 2 (4 OXO 4 (THIOPEN 2 YL)BUTANOYL] 1,2,3,4 TETRAHYDROISOQUINOLINE 3 CARBOXAMIDO] HEXAN 2 YL]CARBAMATE; TERT BUTYL [ 1 [(2,2 DIPHENYLETHYL)AMINO] 1 OXO 6 [ 2 (4 OXO 4 PHENYLBUTANOYL) 1,2,3,4 TETRAHYDROISOQUINOLINE 3 CARBOXAMIDO]HEXAN 2 YL]CARBAMATE; TERT BUTYL [ 1 [(2,2 DIPHENYLETHYL)AMINO] 1 OXO 6 [ 2 (4 OXOPENTANOYL) 1,2,3,4 TETRAHYDROISOQUINOLINE 3 CARBOXAMIDO]HEXAN 2 YL]CARBAMATE; TERT BUTYL [ 1 [(2,2 DIPHENYLETHYL)AMINO] 1 OXO 6 [ 2 [4 OXO 4 (PIPERIDIN 1 YL)BUTANOYL] 1,2,3,4 TETRAHYDROISOQUINOLINE 3 CARBOXAMIDO] 1 OXOHEXAN 2 YL]CARBAMATE; TERT BUTYL [ 1 [(2,2 DIPHENYLETHYL)AMINO] 1 OXO 6 [ 2 [4 OXO 4 (THIOPEN 2 YL)BUTANOYL] 1,2,3,4 TETRAHYDROISOQUINOLINE 3 CARBOXAMIDO]HEXAN 2 YL]CARBAMATE; TERT BUTYL [ 1 [(2,2 DIPHENYLETHYL)AMINO] 6 [ 2 (4 MORPHOLINO 4 OXOBUTANOYL) 1,2,3,4 TETRAHYDROISOQUINOLINE 3 CARBOXAMIDO] 1 OXOHEXAN 2 YL]CARBAMATE; TERT BUTYL [ 1 [(2,2 DIPHENYLETHYL)AMINO] 6 [ 2 [4 (4 FLUOROPHENYL) 4 OXOBUTANOYL] 1,2,3,4 TETRAHYDROISOQUINOLINE 3 CARBOXAMIDO] 1 OXOHEXAN 2 YL]CARBAMATE; TERT BUTYL [ 1 [(2,2 DIPHENYLETHYL)AMINO] 6 [ 2 [4 (4 METHOXYPHENYL) 4 OXOBUTANOYL] 1,2,3,4 TETRAHYDROISOQUINOLINE 3 CARBOXAMIDO] 1 OXOHEXAN 2 YL]CARBAMATE; TERT BUTYL [ 1 [(2,2 DIPHENYLETHYL)AMINO] 6 [ 2 [4 (4 METHYLSULFONYL)PHENYL] 4 OXOBUTANOYL] 1,2,3,4 TETRAHYDROISOQUINOLINE 3 CARBOXAMIDO] 1 OXOHEXAN 2 YL]CARBAMATE; TERT BUTYL [ 1 [(2,2 DIPHENYLETHYL)AMINO] 6 [ 2 [4 (FURAN 2 YL) 4 OXOBUTANOYL] 1,2,3,4 TETRAHYDROISOQUINOLINE 3 CARBOXAMIDO] 1 OXOHEXAN 2 YL]CARBAMATE; TERT BUTYL [ 6 [ 2 [4 (3,4 DIMETHOXYPHENYL) 4 OXOBUTANOYL] 1,2,3,4 TETRAHYDROISOQUINOLINE 3 CARBOXAMIDO] 1 [(2,2 DIPHENYLETHYL)AMINO] 1 OXOHEXAN 2 YL]CARBAMATE; TERT BUTYL [ 6 [(2,2 DIPHENYLETHYL)AMINO] 6 OXO 5 [ 2 (4 OXO 4 PHENYLBUTANOYL) 1,2,3,4 TETRAHYDROISOQUINOLINE 3 CARBOXAMIDO]HEXYL]CARBAMATE; TERT BUTYL [6 AMINO 1 [(2,2 DIPHENYLETHYL)AMINO] 1 OXOHEXAN 2 YL]CARBAMATE; TETRAHYDROISOQUINOLINE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG; CHEMOKINE RECEPTOR CXCR3; CXCR3 PROTEIN, HUMAN; LIGAND;

ALLOSTERISM; ARTICLE; CHEMOTAXIS; CONTROLLED STUDY; DRUG CYTOTOXICITY; DRUG DESIGN; DRUG POTENCY; DRUG SYNTHESIS; HUMAN; HUMAN CELL; INTERNALIZATION; STRUCTURE ACTIVITY RELATION; AGONISTS; ANIMAL; CELL MOTION; CHEMICAL STRUCTURE; CHEMISTRY; CHLOROCEBUS AETHIOPS; COS 1 CELL LINE; DOSE RESPONSE; DRUG DEVELOPMENT; DRUG EFFECTS; HEK293 CELL LINE; METABOLISM; SYNTHESIS;

ALLOSTERIC REGULATION; ANIMALS; CELL MOVEMENT; CERCOPITHECUS AETHIOPS; COS CELLS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; HEK293 CELLS; HUMANS; LIGANDS; MOLECULAR STRUCTURE; RECEPTORS, CXCR3; STRUCTURE-ACTIVITY RELATIONSHIP; TETRAHYDROISOQUINOLINES;

EID: 84961172231     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b01965     Document Type: Article

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