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. Author manuscript; available in PMC: 2011 Jul 21.
Published in final edited form as: Bioconjug Chem. 2010 Jul 21;21(7):1190–1205. doi: 10.1021/bc900569u

Table 1.

Pharmacological data for inhibition of radioligand binding at the hP2Y1 receptor by the novel nucleotide derivatives.

graphic file with name nihms-215911-t0001.jpg

Compound R Binding, Ki, nMa,b
2 I 0.78 ± 0.08 (18)
3 C≡CH 95 ± 39 (18)
4 C≡C(CH2)3CH3 430 ± 200 (18)
5 C≡C(CH2)2COOCH3 363 ± 18
6 C≡C(CH2)3COOCH3 2200 ± 770
7 C≡C(CH2)4COOCH3 649 ± 57
8 C≡C(CH2)2COOH 23 ± 3
9 C≡C(CH2)3COOH 376 ± 101
10 C≡C(CH2)4COOH 350 ± 139
11 C≡C(CH2)2CONH(CH2)2NH2 1440 ± 30
12 C≡C(CH2)3CONH(CH2)2NH2 1150 ± 100
13 C≡C(CH2)4CONH(CH2)2NH2 3960 ± 960
14 C≡C(CH2)2CONH(CH2)3NH2 3580 ± 140
15 C≡C(CH2)2CONH(CH2)4NH2 132 ± 17
16 C≡C(CH2)2CONH(CH2)6NH2 2410 ± 460
17 C≡C(CH2)3CONH(CH2)2NH-biotin >10,000
18 C≡C(CH2)3CONH(CH2)2NHCO(CH2)5NH-biotin 1210 ± 230
19 C≡C(CH2)3CONH(CH2)2-(4-SO2F)-Ph >10,000
20 graphic file with name nihms-215911-t0002.jpg 300 ± 200
21 graphic file with name nihms-215911-t0003.jpg 2700 ± 600
22 graphic file with name nihms-215911-t0004.jpg 8300 ± 1500
23 graphic file with name nihms-215911-t0005.jpg 6300 ± 2000
a

Affinities determined by using [125I]MRS2500 2 in a radioligand binding assay, except for 2 – 4, which were determined using [3H]MRS2279. The hP2Y1 receptor was expressed to high levels in Sf9 insect cells with a recombinant baculovirus. Membranes prepared from these cells were incubated for 30 min at 4°C in the presence of ~1 nM [125I]MRS2500 2.

b

Mean ± standard error given for three separate determinations.

c

2, MRS2500; 8, MRS2816; 15, MRS2900; 20, MRS2939.