-
3
-
-
64249087770
-
-
S.D. Kuduk , C.N. Di Marco , R.K. Chang , R.M. Di Pardo , S.P. Cook , M.J. Cato , A. Jovanovska , M.O. Urban , M. Leitl , R.H. Spencer , S.A. Kane , M.T. Bilodeau , G.D. Hartman , and M.G. Bock Bioorg. Med. Chem. Lett. 19 2009 2514
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 2514
-
-
Kuduk, S.D.1
Di Marco, C.N.2
Chang, R.K.3
Di Pardo, R.M.4
Cook, S.P.5
Cato, M.J.6
Jovanovska, A.7
Urban, M.O.8
Leitl, M.9
Spencer, R.H.10
Kane, S.A.11
Bilodeau, M.T.12
Hartman, G.D.13
Bock, M.G.14
-
4
-
-
67649949741
-
-
S.D. Kuduk , R.K. Chang , J.M.-C. Wai , C.N. Di Marco , V. Cofre , R.M. Di Pardo , S.P. Cook , M.J. Cato , A. Jovanovska , M.O. Urban , M. Leitl , R.H. Spencer , S.A. Kane , G.D. Hartman , and M.T. Bilodeau Bioorg. Med. Chem. Lett. 19 2009 4059
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 4059
-
-
Kuduk, S.D.1
Chang, R.K.2
Wai, J.M.-C.3
Di Marco, C.N.4
Cofre, V.5
Di Pardo, R.M.6
Cook, S.P.7
Cato, M.J.8
Jovanovska, A.9
Urban, M.O.10
Leitl, M.11
Spencer, R.H.12
Kane, S.A.13
Hartman, G.D.14
Bilodeau, M.T.15
-
5
-
-
28844491316
-
-
G.R. Dube , S.G. Lehto , N.M. Breese , S.J. Baker , X. Wang , M.A. Matulenko , P. Honore , A.O. Stewart , R.B. Moreland , and J.D. Brioni Pain 117 2005 88
-
(2005)
Pain
, vol.117
, pp. 88
-
-
Dube, G.R.1
Lehto, S.G.2
Breese, N.M.3
Baker, S.J.4
Wang, X.5
Matulenko, M.A.6
Honore, P.7
Stewart, A.O.8
Moreland, R.B.9
Brioni, J.D.10
-
6
-
-
77952228354
-
-
S.D. Kuduk , C.N. Di Marco , V. Bodmer-Narkevitch , S.P. Cook , M.J. Cato , A. Jovanovska , M.O. Urban , M. Leitl , N. Sain , A. Liang , R.H. Spencer , S.A. Kane , G.D. Hartman , and M.T. Bilodeau ACS Chem. Neurosci. 1 2009 19
-
(2009)
ACS Chem. Neurosci.
, vol.1
, pp. 19
-
-
Kuduk, S.D.1
Di Marco, C.N.2
Bodmer-Narkevitch, V.3
Cook, S.P.4
Cato, M.J.5
Jovanovska, A.6
Urban, M.O.7
Leitl, M.8
Sain, N.9
Liang, A.10
Spencer, R.H.11
Kane, S.A.12
Hartman, G.D.13
Bilodeau, M.T.14
-
7
-
-
79955463077
-
-
This proprietary fragment library complies with typical fragment criteria: average MW 211, A log P 1.4, PSA 40. See Refs. 1 and 8. Importantly, measured aqueous solubilities of the fragments in the library were generally >0.8 mM enabling high concentration screening
-
This proprietary fragment library complies with typical fragment criteria: average MW 211, A log P 1.4, PSA 40. See Refs. 1 and 8. Importantly, measured aqueous solubilities of the fragments in the library were generally >0.8 mM enabling high concentration screening.
-
-
-
-
11
-
-
79955472448
-
-
note
-
50 values were determined by fitting 5-pt titration data to the Hill equation. Up to 2% DMSO could be applied as vehicle with no effect on current magnitude or kinetics. Control compounds (e.g., amiloride) demonstrated similar potency on the PX instrument as we obtained by manual patch clamp electrophysiology.
-
-
-
-
13
-
-
79955469975
-
-
At this point, hits containing the known ASIC3 potency-conferring amidine substructure were removed due to concerns over poor physical properties. See Refs. 3-6
-
At this point, hits containing the known ASIC3 potency-conferring amidine substructure were removed due to concerns over poor physical properties. See Refs. 3-6 .
-
-
-
-
15
-
-
79955468407
-
-
Substitution and modification of the 4-amino group was not planned due to SAR findings from a related series. See the comparison below for an example
-
Substitution and modification of the 4-amino group was not planned due to SAR findings from a related series. See the comparison below for an example.
-
-
-
|