The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27692854 |
100 |
N-Arylsulfonyl-a-amino carboxamides are potent and selective inhibitors of the chemokine receptor CCR10 that show efficacy in the murine DNFB model of contact hypersensitivity. |
Boehringer Ingelheim Pharmaceuticals |
26631321 |
37 |
Discovery and synthesis of cyclohexenyl derivatives as modulators of CC chemokine receptor 2 activity. |
Bristol-Myers Squibb |
25766632 |
31 |
Synthesis and biological evaluation of spirocyclic antagonists of CCR2 (chemokine CC receptor subtype 2). |
Westf£Lische Wilhelms-Universit£T M£Nster |
25893046 |
77 |
Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5. |
Bristol-Myers Squibb |
25666912 |
39 |
When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as CCR2 antagonists. |
Leiden University |
25453791 |
5 |
Design and synthesis of novel small molecule CCR2 antagonists: evaluation of 4-aminopiperidine derivatives. |
TBA |
24685539 |
44 |
The discovery and SAR of cyclopenta[b]furans as inhibitors of CCR2. |
Janssen Research And Development |
24613378 |
33 |
Alkylsulfone-containing trisubstituted cyclohexanes as potent and bioavailable chemokine receptor 2 (CCR2) antagonists. |
Bristol-Myers Squibb |
23916257 |
54 |
Discovery and SAR of 5-aminooctahydrocyclopentapyrrole-3a-carboxamides as potent CCR2 antagonists. |
Janssen Research And Development |
24900633 |
11 |
Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors. |
Amgen |
24900677 |
8 |
Targeting CCR2 Receptor To Treat Inflammation Diseases and Disorders. |
Therachem Research Medilab (India) |
23294701 |
49 |
A novel series of N-(azetidin-3-yl)-2-(heteroarylamino)acetamide CCR2 antagonists. |
Janssen Research And Development |
23182090 |
92 |
Novel 2-aminooctahydrocyclopentalene-3a-carboxamides as potent CCR2 antagonists. |
Janssen Research And Development |
20493592 |
25 |
Validated QSAR analysis of some diaryl substituted pyrazoles as CCR2 inhibitors by various linear and nonlinear multivariate chemometrics methods. |
Tehran University Of Medical Sciences |
20627722 |
89 |
Identification of a sulfonamide series of CCR2 antagonists. |
Glaxosmithkline |
23079519 |
86 |
In vivo activity of an azole series of CCR2 antagonists. |
Glaxosmithkline |
24900425 |
72 |
Discovery of a 4-Azetidinyl-1-thiazoyl-cyclohexane CCR2 Antagonist as a Development Candidate. |
TBA |
23075267 |
85 |
Discovery and lead optimization of a novel series of CC chemokine receptor 1 (CCR1)-selective piperidine antagonists via parallel synthesis. |
Bristol-Myers Squibb |
22931505 |
69 |
Chemokine receptor antagonists. |
National Heart And Lung Institute |
22939233 |
23 |
Benzimidazoles as benzamide replacements within cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists. |
Bristol-Myers Squibb |
22608963 |
109 |
The design and synthesis of novel, potent and orally bioavailable N-aryl piperazine-1-carboxamide CCR2 antagonists with very high hERG selectivity. |
Astrazeneca |
24900280 |
81 |
Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist. |
TBA |
22475558 |
82 |
Discovery of an orally-bioavailable CC Chemokine Receptor 2 antagonist derived from an acyclic diaminoalcohol backbone. |
Bristol-Myers Squibb |
18487045 |
35 |
Substituted dipiperidine alcohols as potent CCR2 antagonists. |
Johnson & Johnson Pharmaceutical Research And Development |
18313297 |
107 |
Potent antagonists of the CCR2b receptor. Part 3: SAR of the (R)-3-aminopyrrolidine series. |
Deltagen Research Laboratories (Former Combichem) |
18215519 |
4 |
Conformational studies of 3-amino-1-alkyl-cyclopentane carboxamide CCR2 antagonists leading to new spirocyclic antagonists. |
Merck Research Laboratories |
18232650 |
35 |
Discovery of disubstituted cyclohexanes as a new class of CC chemokine receptor 2 antagonists. |
TBA |
17046269 |
86 |
Design and synthesis of Rho kinase inhibitors (II). |
Kirin Brewery |
16821774 |
86 |
Design, synthesis, and biological evaluation of the combinatorial library with a new spirodiketopiperazine scaffold. Discovery of novel potent and selective low-molecular-weight CCR5 antagonists. |
Ono Pharmaceutical |
16198561 |
99 |
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis. |
Novartis Institutes For Biomedical Research |
11931608 |
17 |
Inhibition of protein-protein association by small molecules: approaches and progress. |
Pfizer |
24900329 |
49 |
Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist. |
TBA |
22225639 |
29 |
Synthesis of 3-phenylsulfonylmethyl cyclohexylaminobenzamide-derived antagonists of CC chemokine receptor 2 (CCR2). |
Bristol-Myers Squibb |
22061641 |
49 |
The discovery of novel cyclohexylamide CCR2 antagonists. |
Johnson & Johnson Pharmaceutical Research And Development |
22047688 |
51 |
CCR2 receptor antagonists: optimization of biaryl sulfonamides to increase activity in whole blood. |
Glaxosmithkline |
21940167 |
12 |
Design and synthesis of a library of chemokine antagonists. |
Novartis Institutes Of Biomedical Research |
21917454 |
159 |
Design, synthesis and SAR of indazole and benzoisoxazole containing 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists. |
Johnson & Johnson Pharmaceutical Research And Development |
21783361 |
90 |
Overcoming hERG activity in the discovery of a series of 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists. |
Johnson & Johnson Pharmaceutical Research And Development |
21315584 |
74 |
Discovery of ((1S,3R)-1-isopropyl-3-((3S,4S)-3-methoxy-tetrahydro-2H-pyran-4-ylamino)cyclopentyl)(4-(5-(trifluoromethyl)pyridazin-3-yl)piperazin-1-yl)methanone, PF-4254196, a CCR2 antagonist with an improved cardiovascular profile. |
Pfizer |
21341682 |
37 |
Discovery, optimization, and pharmacological characterization of novel heteroaroylphenylureas antagonists of C-C chemokine ligand 2 function. |
Telik |
21316220 |
34 |
Design and synthesis of novel CCR2 antagonists: investigation of non-aryl/heteroaryl binding motifs. |
Pfizer |
21295478 |
81 |
Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist. |
Incyte |
21036044 |
43 |
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. |
Incyte |
20346664 |
27 |
gamma-Lactams as glycinamide replacements in cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists. |
Bristol-Myers Squibb |
20297846 |
33 |
Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication. |
Genzyme |
20223662 |
174 |
Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists. |
Yangji Chemicals |
19674898 |
31 |
Spiropiperidine CCR5 antagonists. |
Roche Palo Alto |
19481449 |
51 |
Novel sulfone-containing di- and trisubstituted cyclohexanes as potent CC chemokine receptor 2 (CCR2) antagonists. |
Bristol-Myers Squibb |
19237282 |
47 |
Design, synthesis, and structure-activity relationship of novel CCR2 antagonists. |
Merck Research Laboratories |
19131247 |
42 |
Discovery of trisubstituted cyclohexanes as potent CC chemokine receptor 2 (CCR2) antagonists. |
Bristol-Myers Squibb |
19014885 |
32 |
Discovery of a potent, selective and orally bioavailable 3,9-diazaspiro[5.5]undeca-2-one CCR5 antagonist. |
Roche Palo Alto |
18990568 |
15 |
Synthesis and structure-activity relationship of 7-azaindole piperidine derivatives as CCR2 antagonists. |
Johnson & Johnson Pharmaceutical Research And Development |
18722120 |
42 |
Synthesis and evaluation of cis-3,4-disubstituted piperidines as potent CC chemokine receptor 2 (CCR2) antagonists. |
Bristol-Myers Squibb |
17715128 |
6 |
Allosteric transinhibition by specific antagonists in CCR2/CXCR4 heterodimers. |
Université |
18258426 |
47 |
QSAR studies on CCR2 antagonists with chiral sensitive hologram descriptors. |
National Institute Of Pharmaceutical Education And Research (Niper) |
18226895 |
29 |
Probing the structural and topological requirements for CCR2 antagonism: holographic QSAR for indolopiperidine derivatives. |
National Institute Of Pharmaceutical Education And Research (Niper) |
18164199 |
34 |
Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists. |
Merck Research Laboratories |
17929797 |
34 |
Synthesis, structure-activity relationship and in vivo antiinflammatory efficacy of substituted dipiperidines as CCR2 antagonists. |
Johnson & Johnson Pharmaceutical Research And Development |
17869105 |
42 |
Synthesis and biological evaluation of phenyl piperidine derivatives as CCR2 antagonists. |
Johnson & Johnson Pharmaceutical Research And Development |
17720492 |
107 |
Capped diaminopropionamide-glycine dipeptides are inhibitors of CC chemokine receptor 2 (CCR2). |
Bristol-Myers Squibb |
17587570 |
34 |
Potent and selective CC-chemokine receptor-2 (CCR2) antagonists as a potential treatment for asthma. |
Johnson & Johnson Pharmaceutical Research And Development |
17482462 |
60 |
3-Amino-1-alkyl-cyclopentane carboxamides as small molecule antagonists of the human and murine CC chemokine receptor 2. |
Merck Research Laboratories |
17461566 |
11 |
Discovery of 3-piperidinyl-1-cyclopentanecarboxamide as a novel scaffold for highly potent CC chemokine receptor 2 antagonists. |
Merck Research Laboratories |
17092717 |
59 |
Alpha-aminothiazole-gamma-aminobutanoic amides as potent, small molecule CCR2 receptor antagonists. |
Merck Research Laboratories |
17088058 |
40 |
Diaryl substituted pyrazoles as potent CCR2 receptor antagonists. |
Merck Research Laboratories |
17084087 |
36 |
Design and synthesis of rho kinase inhibitors (III). |
Kirin Brewery |
16884289 |
26 |
Novel, orally bioavailable gamma-aminoamide CC chemokine receptor 2 (CCR2) antagonists. |
Merck Research Laboratories |
16870431 |
54 |
4-Amino-2-alkyl-butyramides as small molecule CCR2 antagonists with favorable pharmacokinetic properties. |
Merck Research Laboratories |
16698264 |
37 |
Discovery of 3,5-bis(trifluoromethyl)benzyl L-arylglycinamide based potent CCR2 antagonists. |
Merck Research Laboratories |
16539392 |
29 |
Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety. |
Takeda Pharmaceutical |
15863339 |
29 |
Identification of chemokine receptor CCR4 antagonist. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15771462 |
125 |
Discovery of CC chemokine receptor-3 (CCR3) antagonists with picomolar potency. |
Pharmaceutical Research Institute |
15454236 |
36 |
Small molecule antagonists of the CCR2b receptor. Part 2: Discovery process and initial structure-activity relationships of diamine derivatives. |
Deltagen Research Laboratories |
15454235 |
29 |
Small molecule inhibitors of the CCR2b receptor. Part 1: Discovery and optimization of homopiperazine derivatives. |
Institute For Bio-Medical Research |
14698169 |
53 |
N-Benzylindole-2-carboxylic acids: potent functional antagonists of the CCR2b chemokine receptor. |
Astrazeneca |
12954060 |
4 |
CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. |
Glaxosmithkline |
11720852 |
51 |
Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection. |
Merck Research Laboratories |
11720851 |
52 |
Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection. |
Merck Research Laboratories |
11514164 |
36 |
Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists. |
Glaxosmithkline |
11311066 |
76 |
Design, synthesis, and discovery of a novel CCR1 antagonist. |
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories |
11206474 |
51 |
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: structure-activity relationships for substituted 2-Aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes. |
Merck Research Laboratories |
10969972 |
39 |
CCR2B receptor antagonists: conversion of a weak HTS hit to a potent lead compound. |
Smithkline Beecham Pharmaceuticals |
10821717 |
29 |
Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety. |
Takeda Chemical Industries |
18588282 |
63 |
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. |
Johnson & Johnson Pharmaceutical |