-
1
-
-
34247855761
-
Chemokine: Receptor structure, interactions, and antagonism
-
Allen, S. J.; Crown, S. E.; Handel, T. M. Chemokine: receptor structure, interactions, and antagonism Annu. Rev. Immunol. 2007, 25, 787-820
-
(2007)
Annu. Rev. Immunol.
, vol.25
, pp. 787-820
-
-
Allen, S.J.1
Crown, S.E.2
Handel, T.M.3
-
2
-
-
3342990862
-
CCR1 antagonists for the treatment of autoimmune diseases
-
Gladue, R. P.; Zwillich, S. H.; Clucas, A. T.; Brown, M. F. CCR1 antagonists for the treatment of autoimmune diseases Curr. Opin. Invest. Drugs 2004, 5, 499-504
-
(2004)
Curr. Opin. Invest. Drugs
, vol.5
, pp. 499-504
-
-
Gladue, R.P.1
Zwillich, S.H.2
Clucas, A.T.3
Brown, M.F.4
-
3
-
-
36348988548
-
MLN3897, a novel CCR1 inhibitor, impairs osteoclastogenesis and inhibits the interaction of multiple myeloma cells and osteoclasts
-
Vallet, S.; Raje, N.; Ishitsuka, K.; Hideshima, T.; Podar, K.; Chhetri, S.; Possi, S.; Breitkreutz, I.; Kiziltepe, T.; Yasui, H.; Ocio, E. M.; Shiraishi, N.; Jin, J.; Okawa, Y.; Ikeda, H.; Mukherjee, S.; Vaghela, N.; Cirstea, D.; Ladetto, M.; Boccadoro, M.; Anderson, K. C. MLN3897, a novel CCR1 inhibitor, impairs osteoclastogenesis and inhibits the interaction of multiple myeloma cells and osteoclasts Blood 2007, 110, 3744-3752
-
(2007)
Blood
, vol.110
, pp. 3744-3752
-
-
Vallet, S.1
Raje, N.2
Ishitsuka, K.3
Hideshima, T.4
Podar, K.5
Chhetri, S.6
Possi, S.7
Breitkreutz, I.8
Kiziltepe, T.9
Yasui, H.10
Ocio, E.M.11
Shiraishi, N.12
Jin, J.13
Okawa, Y.14
Ikeda, H.15
Mukherjee, S.16
Vaghela, N.17
Cirstea, D.18
Ladetto, M.19
Boccadoro, M.20
Anderson, K.C.21
more..
-
4
-
-
58849121854
-
Chemokine receptor CCR1 regulates inflammatory cell infiltration after renal ischemia-reperfusion injury
-
Furuichi, K.; Gao, J.-L.; Horuk, R.; Wada, T.; Kaneko, S.; Murphy, P. M. Chemokine receptor CCR1 regulates inflammatory cell infiltration after renal ischemia-reperfusion injury J. Immunol. 2008, 181, 8670-8676
-
(2008)
J. Immunol.
, vol.181
, pp. 8670-8676
-
-
Furuichi, K.1
Gao, J.-L.2
Horuk, R.3
Wada, T.4
Kaneko, S.5
Murphy, P.M.6
-
5
-
-
79955476625
-
Overcoming hurdles in developing successful drugs targeting chemokine receptors
-
Schall, T. J.; Proudfoot, A. E. Overcoming hurdles in developing successful drugs targeting chemokine receptors Nat. Rev. Immunol. 2011, 11, 355-363
-
(2011)
Nat. Rev. Immunol.
, vol.11
, pp. 355-363
-
-
Schall, T.J.1
Proudfoot, A.E.2
-
6
-
-
80054935464
-
Targeting CCR1
-
Smit, M. J. Lira, S. A. Leurs, R. Wiley-VCH: Weinheim, Germany
-
Horuk, R. Targeting CCR1. Chemokine Receptors as Drug Targets; Smit, M. J.; Lira, S. A.; Leurs, R., Eds.; Wiley-VCH: Weinheim, Germany, 2011; pp 323-338.
-
(2011)
Chemokine Receptors As Drug Targets
, pp. 323-338
-
-
Horuk, R.1
-
8
-
-
77955631528
-
CCR1 antagonists: What have we learned from clinical trials
-
Gladue, R. P.; Brown, M. F.; Zwillich, S. H. CCR1 antagonists: what have we learned from clinical trials Curr. Top. Med. Chem. 2010, 10, 1268-1277
-
(2010)
Curr. Top. Med. Chem.
, vol.10
, pp. 1268-1277
-
-
Gladue, R.P.1
Brown, M.F.2
Zwillich, S.H.3
-
9
-
-
77958457972
-
N-aryl pyrazoles, indazoles and azaindazoles as antagonists of CC chemokine receptor 1: Patent cooperation treaty applications WO2010/036632, WO2009/134666 and WO2009/137338
-
Carter, P. H.; Hynes, J. N-aryl pyrazoles, indazoles and azaindazoles as antagonists of CC chemokine receptor 1: patent cooperation treaty applications WO2010/036632, WO2009/134666 and WO2009/137338 Expert Opin. Ther. Pat. 2010, 20, 1609-1618
-
(2010)
Expert Opin. Ther. Pat.
, vol.20
, pp. 1609-1618
-
-
Carter, P.H.1
Hynes, J.2
-
10
-
-
77956172932
-
Novel pyrrolidine heterocycles as CCR1 antagonists
-
Merritt, J. R.; James, R.; Paradkar, V. M.; Zhang, C.; Liu, R.; Liu, J.; Jacob, B.; Chiriac, C.; Ohlmeyer, M. J.; Quadros, E.; Wines, P.; Postelnek, J.; Hicks, C. M.; Chen, W.; Kimble, E. F.; O'Brien, L.; White, N.; Desai, H.; Appell, K. C.; Webb, M. L. Novel pyrrolidine heterocycles as CCR1 antagonists Bioorg. Med. Chem. Lett. 2010, 20, 5477-5479
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 5477-5479
-
-
Merritt, J.R.1
James, R.2
Paradkar, V.M.3
Zhang, C.4
Liu, R.5
Liu, J.6
Jacob, B.7
Chiriac, C.8
Ohlmeyer, M.J.9
Quadros, E.10
Wines, P.11
Postelnek, J.12
Hicks, C.M.13
Chen, W.14
Kimble, E.F.15
O'Brien, L.16
White, N.17
Desai, H.18
Appell, K.C.19
Webb, M.L.20
more..
-
11
-
-
0034705618
-
Identification and characterization of a potent, selective and orally active antagonist of the CC Chemokine Receptor-1
-
Liang, M.; Mallari, C.; Rosser, M.; Ng, H. P.; May, K.; Monahan, S.; Bauman, J. G.; Islam, I.; Ghannam, A.; Buckman, B.; Shaw, K.; Wei, G. P.; Xu, W.; Zhao, Z.; Ho, E.; Shen, J.; Oanh, H.; Subramanyam, B.; Vergona, R.; Taub, D.; Dunning, L.; Harvey, S.; Snider, R. M.; Hesselgesser, J.; Morrissey, M. M.; Perez, H. D.; Horuk, R. Identification and characterization of a potent, selective and orally active antagonist of the CC Chemokine Receptor-1 J. Biol. Chem. 2000, 275, 19000-19008
-
(2000)
J. Biol. Chem.
, vol.275
, pp. 19000-19008
-
-
Liang, M.1
Mallari, C.2
Rosser, M.3
Ng, H.P.4
May, K.5
Monahan, S.6
Bauman, J.G.7
Islam, I.8
Ghannam, A.9
Buckman, B.10
Shaw, K.11
Wei, G.P.12
Xu, W.13
Zhao, Z.14
Ho, E.15
Shen, J.16
Oanh, H.17
Subramanyam, B.18
Vergona, R.19
Taub, D.20
Dunning, L.21
Harvey, S.22
Snider, R.M.23
Hesselgesser, J.24
Morrissey, M.M.25
Perez, H.D.26
Horuk, R.27
more..
-
12
-
-
33845458609
-
Blockade of chemokine signaling in patients with multiple sclerosis
-
Zipp, F.; Hartung, H.-P.; Hillert, J.; Schimrigk, S.; Trebst, C.; Stangel, M.; Infante-Duarte, C.; Jakobs, P.; Wolf, C.; Sandbrink, R.; Pohl, C.; Filippi, M. Blockade of chemokine signaling in patients with multiple sclerosis Neurology 2006, 67, 1880-1883
-
(2006)
Neurology
, vol.67
, pp. 1880-1883
-
-
Zipp, F.1
Hartung, H.-P.2
Hillert, J.3
Schimrigk, S.4
Trebst, C.5
Stangel, M.6
Infante-Duarte, C.7
Jakobs, P.8
Wolf, C.9
Sandbrink, R.10
Pohl, C.11
Filippi, M.12
-
13
-
-
17144435064
-
CP-481,715, a potent and selective CCR1 antagonist with potential therapeutic implications for inflammatory diseases
-
Gladue, R. P.; Tylaska, L. A.; Brissette, W. H.; Lira, P. D.; Kath, J. C.; Poss, C. S.; Brown, M. F.; Paradis, T. J.; Conklyn, M. J.; Ogborne, K. T.; McGlynn, M. A.; Lillie, B. M.; DiRico, A. P.; Mairs, E. N.; McElroy, E. B.; Martin, W. H.; Stock, I. A.; Shepard, R. M.; Showell, H. J.; Neote, K. CP-481,715, a potent and selective CCR1 antagonist with potential therapeutic implications for inflammatory diseases J. Biol. Chem. 2003, 278, 40473-40480
-
(2003)
J. Biol. Chem.
, vol.278
, pp. 40473-40480
-
-
Gladue, R.P.1
Tylaska, L.A.2
Brissette, W.H.3
Lira, P.D.4
Kath, J.C.5
Poss, C.S.6
Brown, M.F.7
Paradis, T.J.8
Conklyn, M.J.9
Ogborne, K.T.10
McGlynn, M.A.11
Lillie, B.M.12
Dirico, A.P.13
Mairs, E.N.14
McElroy, E.B.15
Martin, W.H.16
Stock, I.A.17
Shepard, R.M.18
Showell, H.J.19
Neote, K.20
more..
-
14
-
-
0037660976
-
Chemokine blockade and chronic inflammatory disease: Proof of concept in patients with rheumatoid arthritis
-
It is inferred by the authors and others (ref 18) that CP-481715 is the compound employed in the following study
-
It is inferred by the authors and others (ref 18) that CP-481715 is the compound employed in the following study: Haringman, J. J.; Kraan, M. C.; Smeets, T. J. M.; Zwinderman, A. H.; Tak, P. P. Chemokine blockade and chronic inflammatory disease: proof of concept in patients with rheumatoid arthritis Ann. Rheum. Dis. 2003, 62, 715-721
-
(2003)
Ann. Rheum. Dis.
, vol.62
, pp. 715-721
-
-
Haringman, J.J.1
Kraan, M.C.2
Smeets, T.J.M.3
Zwinderman, A.H.4
Tak, P.P.5
-
15
-
-
53149105176
-
Evaluation of the effect of the specific CCR1 antagonist CP-481715 on the clinical and cellular responses observed following epicutaneous nickel challenge in human subjects
-
Borregaard, J.; Skov, L.; Wang, L.; Ting, N.; Wang, C.; Beck, L. A.; Sonne, J.; Clucas, A. Evaluation of the effect of the specific CCR1 antagonist CP-481715 on the clinical and cellular responses observed following epicutaneous nickel challenge in human subjects Contact Dermatitis 2008, 59, 212-219
-
(2008)
Contact Dermatitis
, vol.59
, pp. 212-219
-
-
Borregaard, J.1
Skov, L.2
Wang, L.3
Ting, N.4
Wang, C.5
Beck, L.A.6
Sonne, J.7
Clucas, A.8
-
16
-
-
74949096245
-
AZD-4818, a chemokine CCR1 antagonist: WO2008103126 and WO2009011653
-
Structure suggested from a patent analysis, as described in: Norman, P. AZD-4818, a chemokine CCR1 antagonist: WO2008103126 and WO2009011653 Expert Opin. Ther. Pat. 2009, 19, 1629-1633
-
(2009)
Expert Opin. Ther. Pat.
, vol.19
, pp. 1629-1633
-
-
Norman, P.1
-
17
-
-
84907467956
-
-
Structure inferred from; PCT Intl. Application WO2010/007408, January 21
-
Structure inferred from Chilvers, K.; Hopes, P.; Langer, T. Intermediates 2-(2-chloro-5-hydroxy-4-methylcarbamoylphenoxy)-2-methylpropionic acid tert-butyl ester and glycidyl benzene sulfonates or salts thereof and the process for preparation of said intermediates, PCT Intl. Application WO2010/007408, January 21, 2010; p 3.
-
(2010)
Intermediates 2-(2-chloro-5-hydroxy-4-methylcarbamoylphenoxy)-2-methylpropionic Acid Tert-butyl Ester and Glycidyl Benzene Sulfonates or Salts Thereof and the Process for Preparation of Said Intermediates
, pp. 3
-
-
Chilvers, K.1
Hopes, P.2
Langer, T.3
-
18
-
-
84907467954
-
-
United States National Library of Medicine lists AZD-4818 as having the CAS number 1003566-93-5: (accessed April 28).
-
United States National Library of Medicine lists AZD-4818 as having the CAS number 1003566-93-5: http://chem.sis.nlm.nih.gov/chemidplus/rn/1003566-93-5 (accessed April 28, 2014).
-
(2014)
-
-
-
19
-
-
84866691792
-
Computational studies of the binding modes of CCR1 antagonists
-
Liu, Y.; Chen, B.; Wei, J. Computational studies of the binding modes of CCR1 antagonists Mol. Simul. 2012, 38, 953-960
-
(2012)
Mol. Simul.
, vol.38
, pp. 953-960
-
-
Liu, Y.1
Chen, B.2
Wei, J.3
-
20
-
-
77955664554
-
Tolerability and efficacy of inhaled AZD4818, a CCR1 antagonist, in moderate to severe COPD patients
-
Kerstjens, H. A.; Bjermer, L.; Eriksson, L.; Dahlstrom, K.; Vestbo, J. Tolerability and efficacy of inhaled AZD4818, a CCR1 antagonist, in moderate to severe COPD patients Respir. Med. 2010, 104, 1297-1303
-
(2010)
Respir. Med.
, vol.104
, pp. 1297-1303
-
-
Kerstjens, H.A.1
Bjermer, L.2
Eriksson, L.3
Dahlstrom, K.4
Vestbo, J.5
-
21
-
-
76749099255
-
Quantitative prediction and clinical observation of a CYP3A inhibitor-based drug-drug interactions with MLN3897, a potent CC Chemokine Receptor 1 antagonist
-
Lu, C.; Balani, S. K.; Qian, M. G.; Prakash, S. R.; Ducray, P. S.; von Moltke, L. L. Quantitative prediction and clinical observation of a CYP3A inhibitor-based drug-drug interactions with MLN3897, a potent CC Chemokine Receptor 1 antagonist J. Pharmacol. Exp. Ther. 2010, 332, 562-568
-
(2010)
J. Pharmacol. Exp. Ther.
, vol.332
, pp. 562-568
-
-
Lu, C.1
Balani, S.K.2
Qian, M.G.3
Prakash, S.R.4
Ducray, P.S.5
Von Moltke, L.L.6
-
22
-
-
73249120669
-
MLN3897 plus methotrexate in patients with rheumatoid arthritis: Safety, efficacy, pharmacokinetics, and pharmacodynamics of an oral CCR1 antagonist in a phase IIa, double-blind, placebo-controlled, randomized, proof-of-concept study
-
Vergunst, C. E.; Gerlag, D. M.; von Moltke, L.; Karol, M.; Wyant, T.; Chi, X.; Matzkin, E.; Leach, T.; Tak, P. P. MLN3897 plus methotrexate in patients with rheumatoid arthritis: safety, efficacy, pharmacokinetics, and pharmacodynamics of an oral CCR1 antagonist in a phase IIa, double-blind, placebo-controlled, randomized, proof-of-concept study Arthritis Rheum. 2009, 60, 3572-3581
-
(2009)
Arthritis Rheum.
, vol.60
, pp. 3572-3581
-
-
Vergunst, C.E.1
Gerlag, D.M.2
Von Moltke, L.3
Karol, M.4
Wyant, T.5
Chi, X.6
Matzkin, E.7
Leach, T.8
Tak, P.P.9
-
23
-
-
2942585608
-
Chemokine blockade: A new era in the treatment of rheumatoid arthritis?
-
Harringman, J. J.; Tak, P. P. Chemokine blockade: a new era in the treatment of rheumatoid arthritis? Arthritis Res. Ther. 2004, 6, 93-97
-
(2004)
Arthritis Res. Ther.
, vol.6
, pp. 93-97
-
-
Harringman, J.J.1
Tak, P.P.2
-
24
-
-
79959776294
-
Why CCR2 and CCR5 blockade failed and why CCR1 blockade might still be effective in the treatment of rheumatoid arthritis
-
Lebre, M. C.; Vergunst, C. E.; Choi, I. Y. K.; Aarrass, S.; Oliveira, A. S. F.; Wyant, T.; Horuk, R.; Reedquist, K. A.; Tak, P. P. Why CCR2 and CCR5 blockade failed and why CCR1 blockade might still be effective in the treatment of rheumatoid arthritis PLoS One 2011, 6, e21772
-
(2011)
PLoS One
, vol.6
, pp. 21772
-
-
Lebre, M.C.1
Vergunst, C.E.2
Choi, I.Y.K.3
Aarrass, S.4
Oliveira, A.S.F.5
Wyant, T.6
Horuk, R.7
Reedquist, K.A.8
Tak, P.P.9
-
25
-
-
84871081339
-
-
The structure has not been formally disclosed, but several patent applications from Chemocentryx claim a single compound. For example, see: U.S. Patent application US 2010/0173911 A1.
-
The structure has not been formally disclosed, but several patent applications from Chemocentryx claim a single compound. For example, see: Li, L.; Pennell, A. M. K.; Zhang, P. 3-(Imidazolyl)-pyrazolo[3,4b]-pyridines, U.S. Patent application US 2010/0173911 A1.
-
3-(Imidazolyl)-pyrazolo[3,4b]-pyridines
-
-
Li, L.1
Pennell, A.M.K.2
Zhang, P.3
-
26
-
-
79955483382
-
Pharmacokinetic and pharmacodynamic evaluation of the novel CCR1 antagonist CCX354 in healthy human subjects: Implications for selection of clinical dose
-
Dairaghi, D. J.; Zhang, P.; Wang, Y.; Seitz, L. C.; Johnson, D. A.; Miao, S.; Ertl, L. S.; Zeng, Y.; Powers, J. P.; Pennell, A. M.; Bekker, P.; Schall, T. J.; Jaen, J. C. Pharmacokinetic and pharmacodynamic evaluation of the novel CCR1 antagonist CCX354 in healthy human subjects: implications for selection of clinical dose Clin. Pharmacol. Ther. 2011, 89, 726-734
-
(2011)
Clin. Pharmacol. Ther.
, vol.89
, pp. 726-734
-
-
Dairaghi, D.J.1
Zhang, P.2
Wang, Y.3
Seitz, L.C.4
Johnson, D.A.5
Miao, S.6
Ertl, L.S.7
Zeng, Y.8
Powers, J.P.9
Pennell, A.M.10
Bekker, P.11
Schall, T.J.12
Jaen, J.C.13
-
27
-
-
84907467949
-
-
(accessed Feb. 7). See trial identifiers NCT01027728, Study to evaluate safety and efficacy of CCX 354-C in subjects with rheumatoid arthritis (CARAT-1), and NCT01242917, A study to evaluate the safety and efficacy of CCX354-C in subjects with rheumatoid arthritis partially responsive to methotrexate therapy (CARAT-2).
-
CCX354 is listed as having completed two clinical trials on www.clinicaltrials.gov (accessed Feb. 7, 2013). See trial identifiers NCT01027728, Study to evaluate safety and efficacy of CCX 354-C in subjects with rheumatoid arthritis (CARAT-1), and NCT01242917, A study to evaluate the safety and efficacy of CCX354-C in subjects with rheumatoid arthritis partially responsive to methotrexate therapy (CARAT-2).
-
(2013)
CCX354 is Listed As Having Completed Two Clinical Trials on
-
-
-
28
-
-
84871089732
-
-
ACR/AHRP Meeting, November 8, Chicago, IL; presentation L11.
-
Tak, P. P.; Balancescu, A.; Tseluyko, V.; Bojin, S.; Drescher, E.; Dairaghi, D.; Miao, S.; Marchesin, V.; Jaen, J.; Bekker, P.; Shall, T. J. Safety and efficacy of oral chemokine receptor 1 antagonist CCX354-C in a phase 2 rheumatoid arthritis study, ACR/AHRP Meeting, November 8, 2011, Chicago, IL; presentation L11.
-
(2011)
Safety and Efficacy of Oral Chemokine Receptor 1 Antagonist CCX354-C in A Phase 2 Rheumatoid Arthritis Study
-
-
Tak, P.P.1
Balancescu, A.2
Tseluyko, V.3
Bojin, S.4
Drescher, E.5
Dairaghi, D.6
Miao, S.7
Marchesin, V.8
Jaen, J.9
Bekker, P.10
Shall, T.J.11
-
29
-
-
85028106569
-
Chemokine receptor CCR1 antagonist CCX354-C treatment for rheumatoid arthritis: CARAT-2, a randomised, placebo controlled clinical trial
-
Tak, P. P.; Balanescu, A.; Tseluyko, V. Chemokine receptor CCR1 antagonist CCX354-C treatment for rheumatoid arthritis: CARAT-2, a randomised, placebo controlled clinical trial Ann. Rheum. Dis. 2012, 72, 337-344
-
(2012)
Ann. Rheum. Dis.
, vol.72
, pp. 337-344
-
-
Tak, P.P.1
Balanescu, A.2
Tseluyko, V.3
-
30
-
-
84870039558
-
Discovery and lead optimization of a novel series of CC chemokine receptor 1 (CCR1)-selective piperidine antagonists via parallel synthesis
-
Cavallaro, C. L.; Briceno, S.; Chen, J.; Cvijic, M. E.; Davies, P.; Hynes, J., Jr.; Liu, R.-Q.; Mandlekar, S.; Rose, A.; Tebben, A.; Van Kirk, K.; Watson, A.; Wu, H.; Yang, G.; Carter, P. Discovery and lead optimization of a novel series of CC chemokine receptor 1 (CCR1)-selective piperidine antagonists via parallel synthesis J. Med. Chem. 2012, 55, 9643-9653
-
(2012)
J. Med. Chem.
, vol.55
, pp. 9643-9653
-
-
Cavallaro, C.L.1
Briceno, S.2
Chen, J.3
Cvijic, M.E.4
Davies, P.5
Hynes, J.6
Liu, R.-Q.7
Mandlekar, S.8
Rose, A.9
Tebben, A.10
Van Kirk, K.11
Watson, A.12
Wu, H.13
Yang, G.14
Carter, P.15
-
31
-
-
84878869013
-
The discovery of BMS-457, a potent and selective CCR1 antagonist
-
Gardner, D. S.; Santella, J. B., III; Duncia, J. V.; Carter, P. H.; Dhar, T. G. M.; Wu, H.; Guo, W.; Cavallaro, C.; Van Kirk, K.; Yarde, M.; Briceno, S. W.; Grafstrom, R. R.; Liu, R.; Patel, S. R.; Tebben, A. J.; Camac, D.; Khan, J.; Watson, A.; Yang, G.; Rose, A.; Foster, W. R.; Cvijic, M. E.; Davies, P.; Hynes, J., Jr. The discovery of BMS-457, a potent and selective CCR1 antagonist Bioorg. Med. Chem. Lett. 2013, 23, 3833-3840
-
(2013)
Bioorg. Med. Chem. Lett.
, vol.23
, pp. 3833-3840
-
-
Gardner, D.S.1
Santella, B.J.2
Duncia, J.V.3
Carter, P.H.4
Dhar, T.G.M.5
Wu, H.6
Guo, W.7
Cavallaro, C.8
Van Kirk, K.9
Yarde, M.10
Briceno, S.W.11
Grafstrom, R.R.12
Liu, R.13
Patel, S.R.14
Tebben, A.J.15
Camac, D.16
Khan, J.17
Watson, A.18
Yang, G.19
Rose, A.20
Foster, W.R.21
Cvijic, M.E.22
Davies, P.23
Hynes, J.24
more..
-
33
-
-
0036799870
-
The nuclear pregnane X receptor: A key regulator of xenobiotic metabolism
-
Kliewer, S.; Goodwin, B.; Willson, T. The nuclear pregnane X receptor: a key regulator of xenobiotic metabolism Endocr. Rev. 2002, 23, 687-702
-
(2002)
Endocr. Rev.
, vol.23
, pp. 687-702
-
-
Kliewer, S.1
Goodwin, B.2
Willson, T.3
-
34
-
-
38349002583
-
From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: The discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis
-
Santella, J. B., III; Gardner, D. S.; Yao, W.; Shi, C.; Reddy, P.; Tebben, A.; Delucca, G. V.; Wacker, D. A.; Watson, P. S.; Welch, P. K.; Wadman, E. A.; Davies, P.; Solomon, K. A.; Graden, D. M.; Yeleswaram, S.; Mandlekar, S.; Kariv, I.; Decicco, C. P.; Ko, S. S.; Carter, P. H.; Duncia, J. V. From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: the discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis Bioorg. Med. Chem. Lett. 2008, 18, 576-585
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 576-585
-
-
Santella, B.J.1
Gardner, D.S.2
Yao, W.3
Shi, C.4
Reddy, P.5
Tebben, A.6
Delucca, G.V.7
Wacker, D.A.8
Watson, P.S.9
Welch, P.K.10
Wadman, E.A.11
Davies, P.12
Solomon, K.A.13
Graden, D.M.14
Yeleswaram, S.15
Mandlekar, S.16
Kariv, I.17
Decicco, C.P.18
Ko, S.S.19
Carter, P.H.20
Duncia, J.V.21
more..
-
35
-
-
22744449063
-
Discovery and preclinical profile of Saxagliptin (BMS-477118): A highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
-
Augeri, D. J.; Robl, J. A.; Betebenner, D. A.; Magnin, D. R.; Khanna, A.; Robertson, J. G.; Wang, A.; Simpkins, L. M.; Taunk, P.; Huang, Q.; Han, S.-P.; Abboa-Offei, B.; Cap, M.; Xin, L.; Tao, L.; Tozzo, E.; Welzel, G. E.; Egan, D. M.; Marcinkeviciene, J.; Chang, S. Y.; Biller, S. A.; Kirby, M. S.; Parker, R. A.; Hamann, L. G. Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes J. Med. Chem. 2005, 48, 5025-5037
-
(2005)
J. Med. Chem.
, vol.48
, pp. 5025-5037
-
-
Augeri, D.J.1
Robl, J.A.2
Betebenner, D.A.3
Magnin, D.R.4
Khanna, A.5
Robertson, J.G.6
Wang, A.7
Simpkins, L.M.8
Taunk, P.9
Huang, Q.10
Han, S.-P.11
Abboa-Offei, B.12
Cap, M.13
Xin, L.14
Tao, L.15
Tozzo, E.16
Welzel, G.E.17
Egan, D.M.18
Marcinkeviciene, J.19
Chang, S.Y.20
Biller, S.A.21
Kirby, M.S.22
Parker, R.A.23
Hamann, L.G.24
more..
-
36
-
-
0035933511
-
The human nuclear xenobiotic receptor PXR: Structural determinants of directed promiscuity
-
Watkins, R. E.; Wisely, G. B.; Moore, L. B. The human nuclear xenobiotic receptor PXR: structural determinants of directed promiscuity Science. 2001, 292, 2329-2333
-
(2001)
Science.
, vol.292
, pp. 2329-2333
-
-
Watkins, R.E.1
Wisely, G.B.2
Moore, L.B.3
-
37
-
-
84907451770
-
PXR: A xenobiotic receptor of diverse function implicated in pharmacogenetics
-
Gillam, E. M. PXR: a xenobiotic receptor of diverse function implicated in pharmacogenetics Trends Pharmacol. Sci. 2001, 22, 448
-
(2001)
Trends Pharmacol. Sci.
, vol.22
, pp. 448
-
-
Gillam, E.M.1
-
38
-
-
0037442002
-
Structure function differences in nonpeptide CCR1 antagonists for human and mouse CCR1
-
Onuffer, J.; McCarrick, M. A.; Dunning, L.; Liang, M.; Rosser, M.; Wei, G.-P.; Ng, H.; Horuk, R. Structure function differences in nonpeptide CCR1 antagonists for human and mouse CCR1 J. Immunol. 2003, 170, 1910-1916
-
(2003)
J. Immunol.
, vol.170
, pp. 1910-1916
-
-
Onuffer, J.1
McCarrick, M.A.2
Dunning, L.3
Liang, M.4
Rosser, M.5
Wei, G.-P.6
Ng, H.7
Horuk, R.8
-
39
-
-
17144435064
-
CP-481,715, a potent and selective CCR1 antagonist with potential therapeutic implications for inflammatory diseases
-
Gladue, R. P.; Tylaska, L. A.; Brissette, W. H.; Lira, P. D.; Kath, J. C.; Poss, C. S.; Brown, M. F.; Paradis, T. J.; Conklyn, M. J.; Ogborne, K. T.; McGlynn, M. A.; Lillie, B. M.; DiRico, A. P.; Mairs, E. N.; McElroy, E. B.; Martin, W. H.; Stock, I. A.; Shepard, R. M.; Showell, H. J.; Neote, K. CP-481,715, a potent and selective CCR1 antagonist with potential therapeutic implications for inflammatory diseases J. Biol. Chem. 2003, 278, 40473-40480
-
(2003)
J. Biol. Chem.
, vol.278
, pp. 40473-40480
-
-
Gladue, R.P.1
Tylaska, L.A.2
Brissette, W.H.3
Lira, P.D.4
Kath, J.C.5
Poss, C.S.6
Brown, M.F.7
Paradis, T.J.8
Conklyn, M.J.9
Ogborne, K.T.10
McGlynn, M.A.11
Lillie, B.M.12
Dirico, A.P.13
Mairs, E.N.14
McElroy, E.B.15
Martin, W.H.16
Stock, I.A.17
Shepard, R.M.18
Showell, H.J.19
Neote, K.20
more..
-
40
-
-
84907467947
-
-
The PDB deposition number is 4NY9.
-
The PDB deposition number is 4NY9.
-
-
-
-
41
-
-
0031059866
-
Processing of X-ray diffraction data collected in oscillation mode
-
Otwinowski, Z.; Minor, W. Processing of X-ray diffraction data collected in oscillation mode Methods Enzymol. 2007, 276, 307-326
-
(2007)
Methods Enzymol.
, vol.276
, pp. 307-326
-
-
Otwinowski, Z.1
Minor, W.2
-
42
-
-
34447508216
-
PHASER crystallographic software
-
McCoy, A. J.; Grosse-Kunstleve, R. W.; Adams, P. D.; Winn, M. D.; Storoni, L. C.; Read, R. J. PHASER crystallographic software J. Appl. Crystallogr. 2007, 40, 658-674
-
(2007)
J. Appl. Crystallogr.
, vol.40
, pp. 658-674
-
-
McCoy, A.J.1
Grosse-Kunstleve, R.W.2
Adams, P.D.3
Winn, M.D.4
Storoni, L.C.5
Read, R.J.6
-
43
-
-
33846627754
-
Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism
-
Xue, Y.; Chao, E.; Zuercher, W. J.; Willson, T. M.; Collins, J. L.; Redinbo, M. R. Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism Bioorg. Med. Chem. 2007, 15, 2156-2166
-
(2007)
Bioorg. Med. Chem.
, vol.15
, pp. 2156-2166
-
-
Xue, Y.1
Chao, E.2
Zuercher, W.J.3
Willson, T.M.4
Collins, J.L.5
Redinbo, M.R.6
-
44
-
-
77949535720
-
Features and development of COOT
-
Emsley, P.; Lohkamp, B.; Scott, W. G.; Cowtan, K. Features and development of COOT Acta Crystallogr., Sect. D: Biol. Crystallogr. 2010, 66, 486-501
-
(2010)
Acta Crystallogr., Sect. D: Biol. Crystallogr.
, vol.66
, pp. 486-501
-
-
Emsley, P.1
Lohkamp, B.2
Scott, W.G.3
Cowtan, K.4
|