| Compound ID |
Compound Name |
Compound Formula |
|
CP0947119
|
6-(4-cyano-2-fluorobenzoyl)-3-methoxy-2-(S)-{1-[4-(trifluoromethyl)phenyl]ethylamino}-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-(3H)-one hydrochloride
Show/Hide
|
C25H22ClF4N5O3
|
2
|
| 1 |
IC50 = 34 nM
|
|
|
| 2 |
Ki = 15 nM
|
|
|
|
CP0556997
|
US9206173, 11
Show/Hide
|
C25H21F4N5O3
|
2
|
| 1 |
IC50 = 34 nM
|
|
|
| 2 |
Ki = 15 nM
|
|
|
|
CP0948123
|
6-(4-cyano-2-fluorobenzoyl)-3-propargyl-2-(S)-{1-[4-(trifluoromethyl)phenyl]ethylamino}-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-(3H)-one hydrochloride
Show/Hide
|
C27H22ClF4N5O2
|
2
|
| 1 |
IC50 = 42 nM
|
|
|
| 2 |
Ki = 5 nM
|
|
|
|
CP0542727
|
US9206173, 1
Show/Hide
|
C27H21F4N5O2
|
2
|
| 1 |
IC50 = 42 nM
|
|
|
| 2 |
Ki = 5 nM
|
|
|
|
CP0861810
|
6-(4-cyano-2-fluorobenzoyl)-3-dimethylamino-2-(S)-{1-[4-(trifluoromethyl)phenyl]ethylamino}-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-(3H)-one hydrochloride
Show/Hide
|
C26H25ClF4N6O2
|
2
|
| 1 |
IC50 = 46 nM
|
|
|
| 2 |
Ki = 8 nM
|
|
|
|
CP0483915
|
US9206173, 5
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|
C26H24F4N6O2
|
2
|
| 1 |
IC50 = 46 nM
|
|
|
| 2 |
Ki = 8 nM
|
|
|
|
CP0903367
|
4-{3-(3-butynyl)-4-oxo-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-3,5,7,8-tetrahydro-4H-pyrido[4,3-d]pyrimidine-6-carbonyl}benzonitrile
Show/Hide
|
C28H24F3N5O2
|
2
|
| 1 |
IC50 = 62 nM
|
|
|
| 2 |
Ki = 5 nM
|
|
|
|
CP0527354
|
US9206173, 2433
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|
C27H23F3N6O2
|
2
|
| 1 |
IC50 = 62 nM
|
|
|
| 2 |
Ki = 5 nM
|
|
|
|
CP0402863
|
US9206173, 2435
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|
C28H23F4N5O2
|
2
|
| 1 |
IC50 = 68 nM
|
|
|
| 2 |
Ki = 2 nM
|
|
|
|
CP0850662
|
4-{3-(2-butynyl)-4-oxo-2-[(S)-1-(4-trifluoromethylphenyl)ethylanino]-3,5,7,8-tetrahydro-4H-pyrido[4,3-d]pyrimidine-6-carbonyl}-3-fluorobenzonitrile hydrochloride
Show/Hide
|
C28H24ClF4N5O2
|
2
|
| 1 |
IC50 = 78 nM
|
|
|
| 2 |
Ki = 2 nM
|
|
|
|
CP0414272
|
US9206173, 2406
Show/Hide
|
C28H23F4N5O2
|
2
|
| 1 |
IC50 = 78 nM
|
|
|
| 2 |
Ki = 2 nM
|
|
|
|
CP0853645
|
3-(2-butynyl)-6-(4-imidazol-1-ylbenzoyl)-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one dihydrochloride
Show/Hide
|
C30H29Cl2F3N6O2
|
2
|
| 1 |
IC50 = 99 nM
|
|
|
| 2 |
Ki = 6 nM
|
|
|
|
CP0483917
|
US9206173, 2402
Show/Hide
|
C30H27F3N6O2
|
2
|
| 1 |
IC50 = 99 nM
|
|
|
| 2 |
Ki = 6 nM
|
|
|
|
CP0853651
|
4-{3-methoxy-4-oxo-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-3,5,7,8-tetrahydro-4H-pyrido[4,3-d]pyrimidine-6-carbonyl}benzonitrile
Show/Hide
|
C25H22F3N5O3
|
2
|
| 1 |
IC50 = 140 nM
|
|
|
| 2 |
Ki = 2 nM
|
|
|
|
CP0880949
|
6-(4-chlorobenzoyl)-3-methoxy-2-(S)-{1-[4-(trifluoromethyl)phenyl]ethylamino}-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-(3H)-one hydrochloride
Show/Hide
|
C24H23Cl2F3N4O3
|
2
|
| 1 |
IC50 = 140 nM
|
|
|
| 2 |
Ki = 17 nM
|
|
|
|
CP0414284
|
US9206173, 2386
Show/Hide
|
C25H22F3N5O3
|
2
|
| 1 |
IC50 = 140 nM
|
|
|
| 2 |
Ki = 2 nM
|
|
|
|
CP0549764
|
US9206173, 10
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|
C24H22ClF3N4O3
|
2
|
| 1 |
IC50 = 140 nM
|
|
|
| 2 |
Ki = 17 nM
|
|
|
|
CP0947120
|
(S)-4-(3-ethoxy-4-oxo-2-(1-(4-(trifluoromethyl)phenyl)ethylamino)-3,4,5,6,7,8-hexahydropyrido[4,3-d]pyrimidine-6-carbonyl)benzonitrile
Show/Hide
|
C26H24F3N5O3
|
2
|
| 1 |
IC50 = 156 nM
|
|
|
| 2 |
Ki = 11 nM
|
|
|
|
CP0567355
|
US9206173, 92
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|
C26H24F3N5O3
|
2
|
| 1 |
IC50 = 156 nM
|
|
|
| 2 |
Ki = 11 nM
|
|
|
|
CP0896897
|
(S)-3-ethoxy-6-(4-(oxazol-5-yl)benzoyl)-2-(1-(4-(trifluoromethyl)phenyl)ethylamino)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one
Show/Hide
|
C28H26F3N5O4
|
2
|
| 1 |
IC50 = 158 nM
|
|
|
| 2 |
Ki = 20 nM
|
|
|
|
CP0556998
|
US9206173, 104
Show/Hide
|
C28H26F3N5O4
|
2
|
| 1 |
IC50 = 158 nM
|
|
|
| 2 |
Ki = 20 nM
|
|
|
|
CP0866469
|
6-(4-chlorobenzoyl)-3-dimethylamino-2-(S)-{1-[4-(trifluoromethyl)phenyl]ethylamino}-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-(3H)-one hydrochloride
Show/Hide
|
C25H26Cl2F3N5O2
|
2
|
| 1 |
IC50 = 187 nM
|
|
|
| 2 |
Ki = 17 nM
|
|
|
|
CP0867896
|
3-fluoro-4-{3-morpholin-4-yl-4-oxo-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-3,5,7,8-tetrahydro-4H-pyrido[4,3-d]pyrimidine-6-carbonyl}benzonitrile hydrochloride
Show/Hide
|
C28H27ClF4N6O3
|
2
|
| 1 |
IC50 = 187 nM
|
|
|
| 2 |
Ki = 3 nM
|
|
|
|
CP0414282
|
US9206173, 6
Show/Hide
|
C25H25ClF3N5O2
|
2
|
| 1 |
IC50 = 187 nM
|
|
|
| 2 |
Ki = 17 nM
|
|
|
|
CP0426266
|
US9206173, 2463
Show/Hide
|
C28H26F4N6O3
|
2
|
| 1 |
IC50 = 187 nM
|
|
|
| 2 |
Ki = 3 nM
|
|
|
|
CP0407276
|
US9206173, 9
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|
C23H22Cl2N4O3
|
2
|
| 1 |
IC50 = 204 nM
|
|
|
| 2 |
Ki = 28 nM
|
|
|
|
CP0853603
|
4-{3-(2-butynyl)-4-oxo-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-3,5,7,8-tetrahydro-4H-pyrido[4,3-d]pyrimidine-6-carbonyl}benzonitrile hydrochloride
Show/Hide
|
C28H25ClF3N5O2
|
2
|
| 1 |
IC50 = 207 nM
|
|
|
| 2 |
Ki = 8 nM
|
|
|
|
CP0522218
|
US9206173, 2407
Show/Hide
|
C28H24F3N5O2
|
2
|
| 1 |
IC50 = 207 nM
|
|
|
| 2 |
Ki = 8 nM
|
|
|
|
CP0958520
|
3-dimethylamino-6-(2,4,6-trifluorobenzoyl)-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one hydrochloride
Show/Hide
|
C25H24ClF6N5O2
|
2
|
| 1 |
IC50 = 216 nM
|
|
|
| 2 |
Ki = 6 nM
|
|
|
|
CP0512083
|
US9206173, 2484
Show/Hide
|
C24H22F6N6O2
|
2
|
| 1 |
IC50 = 216 nM
|
|
|
| 2 |
Ki = 6 nM
|
|
|
|
CP0880950
|
(S)-4-(3-ethoxy-4-oxo-2-(1-(4-(trifluoromethyl)phenyl)ethylamino)-3,4,5,6,7,8-hexahydropyrido[4,3-d]pyrimidine-6-carbonyl)-3-fluorobenzonitrile
Show/Hide
|
C26H23F4N5O3
|
2
|
| 1 |
IC50 = 227 nM
|
|
|
| 2 |
Ki = 5 nM
|
|
|
|
CP0523931
|
US9206173, 95
Show/Hide
|
C26H23F4N5O3
|
2
|
| 1 |
IC50 = 227 nM
|
|
|
| 2 |
Ki = 5 nM
|
|
|
|
CP0896899
|
6-(2,6-dimethoxypyridine-3-carbonyl)-3-methoxy-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C25H26F3N5O5
|
2
|
| 1 |
IC50 = 228 nM
|
|
|
| 2 |
Ki = 7 nM
|
|
|
|
CP0483918
|
US9206173, 2419
Show/Hide
|
C25H26F3N5O5
|
2
|
| 1 |
IC50 = 228 nM
|
|
|
| 2 |
Ki = 7 nM
|
|
|
|
CP0850610
|
4-{3-morpholin-4-yl-4-oxo-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-3,5,7,8-tetrahydro-4H-pyrido[4,3-d]pyrimidine-6-carbonyl}benzonitrile hydrochloride
Show/Hide
|
C28H28ClF3N6O3
|
2
|
| 1 |
IC50 = 238 nM
|
|
|
| 2 |
Ki = 36 nM
|
|
|
|
CP0483914
|
US9206173, 2432
Show/Hide
|
C27H26F3N7O3
|
2
|
| 1 |
IC50 = 238 nM
|
|
|
| 2 |
Ki = 36 nM
|
|
|
|
CP0959626
|
6-(4-chlorobenzoyl)-2-(S)-[1-(4-chlorophenyl)ethylamino]-3-dimethylamino-5,6,7,8-terahydropydo[4,3-d]pyimidin-4-(3H)-one hydrochloride
Show/Hide
|
C24H26Cl3N5O2
|
2
|
| 1 |
IC50 = 253 nM
|
|
|
| 2 |
Ki = 25 nM
|
|
|
|
CP0542729
|
US9206173, 8
Show/Hide
|
C24H25Cl2N5O2
|
2
|
| 1 |
IC50 = 253 nM
|
|
|
| 2 |
Ki = 25 nM
|
|
|
|
CP0871168
|
3-(2-butynyl)-6-(2-oxo-1,2,3,4-tetrahydro-quinoline-6-carbonyl)-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one hydrochloride
Show/Hide
|
C30H29ClF3N5O3
|
2
|
| 1 |
IC50 = 259 nM
|
|
|
| 2 |
Ki = 8 nM
|
|
|
|
CP0519540
|
US9206173, 2412
Show/Hide
|
C30H28F3N5O3
|
2
|
| 1 |
IC50 = 259 nM
|
|
|
| 2 |
Ki = 8 nM
|
|
|
|
CP0852642
|
3-methoxy-6-(quinoline-3-carbonyl)-2-[(S)-1-4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3Hpyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C27H24F3N5O3
|
2
|
| 1 |
IC50 = 286 nM
|
|
|
| 2 |
Ki = 8 nM
|
|
|
|
CP0412647
|
US9206173, 2418
Show/Hide
|
C27H24F3N5O3
|
2
|
| 1 |
IC50 = 286 nM
|
|
|
| 2 |
Ki = 8 nM
|
|
|
|
CP0880935
|
(S)-3-fluoro-4-(4-oxo-3-(pyrrolidin-1-yl)-2-(1-(4-(trifluoromethyl)phenyl)ethylamino)-3,4,5,6,7,8-hexahydropyrido[4,3-d]pyrimidine-6-carbonyl)benzonitrile
Show/Hide
|
C28H26F4N6O2
|
2
|
| 1 |
IC50 = 298 nM
|
|
|
| 2 |
Ki = 6 nM
|
|
|
|
CP0561342
|
US9206173, 166
Show/Hide
|
C28H26F4N6O2
|
2
|
| 1 |
IC50 = 298 nM
|
|
|
| 2 |
Ki = 6 nM
|
|
|
|
CP0947118
|
6-(4-chlorobenzoyl)-3-propargyl-2-(S)-{1-[4-(trifluoromethyl)phenyl]ethylamino}-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-(3H)-one hydrochloride
Show/Hide
|
C26H23Cl2F3N4O2
|
2
|
| 1 |
IC50 = 378 nM
|
|
|
| 2 |
Ki = 29 nM
|
|
|
|
CP0414281
|
US9206173, 2
Show/Hide
|
C26H22ClF3N4O2
|
2
|
| 1 |
IC50 = 378 nM
|
|
|
| 2 |
Ki = 29 nM
|
|
|
|
CP0935557
|
(S)-4-(4-oxo-3-(pyrrolidin-1-yl)-2-(1-(4-(trifluoromethyl)phenyl)ethylamino)-3,4,5,6,7,8-hexahydropyrido[4,3-d]pyrimidine-6-carbonyl)benzonitrile
Show/Hide
|
C28H27F3N6O2
|
2
|
| 1 |
IC50 = 648 nM
|
|
|
| 2 |
Ki = 10 nM
|
|
|
|
CP0483916
|
US9206173, 163
Show/Hide
|
C28H27F3N6O2
|
2
|
| 1 |
IC50 = 648 nM
|
|
|
| 2 |
Ki = 10 nM
|
|
|
|
CP0866471
|
3-(2-butynyl)-6-(4-oxazol-5-ylbenzoyl)-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one hydrochloride
Show/Hide
|
C30H27ClF3N5O3
|
2
|
| 1 |
IC50 = 665 nM
|
|
|
| 2 |
Ki = 10 nM
|
|
|
|
CP0519539
|
US9206173, 2410
Show/Hide
|
C30H26F3N5O3
|
2
|
| 1 |
IC50 = 665 nM
|
|
|
| 2 |
Ki = 10 nM
|
|
|
|
CP0867894
|
6-[2-(4-chlorophenoxy)acetyl]-3-methoxy-2-[(S)-1-(4-tritluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C25H24ClF3N4O4
|
2
|
| 1 |
IC50 = 678 nM
|
|
|
| 2 |
Ki = 8 nM
|
|
|
|
CP0542226
|
US9206173, 2389
Show/Hide
|
C25H24ClF3N4O4
|
2
|
| 1 |
IC50 = 678 nM
|
|
|
| 2 |
Ki = 8 nM
|
|
|
|
CP0861809
|
(S)-3-methoxy-6-(4-(trifluoromethoxy)benzoyl)-2-(1-(4-(trifluoromethyl)phenyl)ethylamino)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one
Show/Hide
|
C25H22F6N4O4
|
2
|
| 1 |
IC50 = 686 nM
|
|
|
| 2 |
Ki = 16 nM
|
|
|
|
CP0565151
|
US9206173, 63
Show/Hide
|
C25H22F6N4O4
|
2
|
| 1 |
IC50 = 686 nM
|
|
|
| 2 |
Ki = 16 nM
|
|
|
|
CP0866470
|
3-(2-butynyl)-6-(pyrazolo[1,5-a]pyridine-2-carbonyl)-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one hydrochloride
Show/Hide
|
C28H26ClF3N6O2
|
2
|
| 1 |
IC50 = 776 nM
|
|
|
| 2 |
Ki = 20 nM
|
|
|
|
CP0559724
|
US9206173, 2411
Show/Hide
|
C28H25F3N6O2
|
2
|
| 1 |
IC50 = 776 nM
|
|
|
| 2 |
Ki = 20 nM
|
|
|
|
CP0860144
|
3-(2-butynyl)-6-(quinoline-7-carbonyl)-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one dihydrochloride
Show/Hide
|
C30H28Cl2F3N5O2
|
2
|
| 1 |
IC50 = 780 nM
|
|
|
| 2 |
Ki = 17 nM
|
|
|
|
CP0414274
|
US9206173, 2417
Show/Hide
|
C30H26F3N5O2
|
2
|
| 1 |
IC50 = 780 nM
|
|
|
| 2 |
Ki = 17 nM
|
|
|
|
CP0903392
|
6-(5-chlorobenzofuran-2-carbonyl)-3-methoxy-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C26H22ClF3N4O4
|
2
|
| 1 |
IC50 = 824 nM
|
|
|
| 2 |
Ki = 12 nM
|
|
|
|
CP0414271
|
US9206173, 2403
Show/Hide
|
C26H22ClF3N4O4
|
2
|
| 1 |
IC50 = 824 nM
|
|
|
| 2 |
Ki = 12 nM
|
|
|
|
CP0947121
|
6-(3,4-dimethylbenzoyl)-3-methoxy-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C26H27F3N4O3
|
2
|
| 1 |
IC50 = 1031 nM
|
|
|
| 2 |
Ki = 4 nM
|
|
|
|
CP0557000
|
US9206173, 2452
Show/Hide
|
C26H27F3N4O3
|
2
|
| 1 |
IC50 = 1031 nM
|
|
|
| 2 |
Ki = 4 nM
|
|
|
|
CP0849090
|
3-methoxy-6-(5-methyl-thiophene-2-carbonyl)-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C23H23F3N4O3S
|
2
|
| 1 |
IC50 = 1128 nM
|
|
|
| 2 |
Ki = 10 nM
|
|
|
|
CP0523932
|
US9206173, 2404
Show/Hide
|
C23H23F3N4O3S
|
2
|
| 1 |
IC50 = 1128 nM
|
|
|
| 2 |
Ki = 10 nM
|
|
|
|
CP0948127
|
6-[2-(4-chlorophenylsulfanyl)acetyl]-3-methoxy-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C25H24ClF3N4O3S
|
2
|
| 1 |
IC50 = 1140 nM
|
|
|
| 2 |
Ki = 8 nM
|
|
|
|
CP0414269
|
US9206173, 2390
Show/Hide
|
C25H24ClF3N4O3S
|
2
|
| 1 |
IC50 = 1140 nM
|
|
|
| 2 |
Ki = 8 nM
|
|
|
|
CP0935558
|
6-[2-(4-chlorophenoxy)acetyl]-2-[(S)-1-(4-chlorophenyl)ethylamino]-3-methoxy-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C24H24Cl2N4O4
|
2
|
| 1 |
IC50 = 1183 nM
|
|
|
| 2 |
Ki = 15 nM
|
|
|
|
CP0567356
|
US9206173, 2430
Show/Hide
|
C24H24Cl2N4O4
|
2
|
| 1 |
IC50 = 1183 nM
|
|
|
| 2 |
Ki = 15 nM
|
|
|
|
CP0911813
|
6-(4-ethoxybenzoyl)-3-methoxy-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C26H27F3N4O4
|
2
|
| 1 |
IC50 = 1285 nM
|
|
|
| 2 |
Ki = 9 nM
|
|
|
|
CP0527355
|
US9206173, 2451
Show/Hide
|
C26H27F3N4O4
|
2
|
| 1 |
IC50 = 1285 nM
|
|
|
| 2 |
Ki = 9 nM
|
|
|
|
CP0904424
|
6-(4-chlorobenzoyl)-2-[1-(4-chlorophenyl)propylamino]-3-methoxy-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one hydrochloride
Show/Hide
|
C24H25Cl3N4O3
|
2
|
| 1 |
IC50 = 1570 nM
|
|
|
| 2 |
Ki = 44 nM
|
|
|
|
CP0412650
|
US9206173, 2421
Show/Hide
|
C24H24Cl2N4O3
|
2
|
| 1 |
IC50 = 1570 nM
|
|
|
| 2 |
Ki = 44 nM
|
|
|
|
CP0857910
|
(S)-3-ethoxy-6-(4-(thieno[2,3-b]pyridin-2-yl)benzoyl)-2-(1-(4-(trifluoromethyl)phenyl)ethylamino)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one
Show/Hide
|
C26H24F3N5O3S
|
2
|
| 1 |
IC50 = 1684 nM
|
|
|
| 2 |
Ki = 17 nM
|
|
|
|
CP0423837
|
US9206173, 121
Show/Hide
|
C26H24F3N5O3S
|
2
|
| 1 |
IC50 = 1684 nM
|
|
|
| 2 |
Ki = 17 nM
|
|
|
|
CP0456490
|
US9206173, 3
Show/Hide
|
C25H22Cl2N4O2
|
2
|
| 1 |
IC50 = 1722 nM
|
|
|
| 2 |
Ki = 42 nM
|
|
|
|
CP0967837
|
6-(4-chloro-3-methylbenzoyl)-3-methoxy-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C25H24ClF3N4O3
|
2
|
| 1 |
IC50 = 2225 nM
|
|
|
| 2 |
Ki = 20 nM
|
|
|
|
CP0567076
|
US9206173, 2396
Show/Hide
|
C25H24ClF3N4O3
|
2
|
| 1 |
IC50 = 2225 nM
|
|
|
| 2 |
Ki = 20 nM
|
|
|
|
CP0866456
|
3-(2-butynyl)-6-(4-chlorobenzoyl)-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one hydrochloride
Show/Hide
|
C27H25Cl2F3N4O2
|
2
|
| 1 |
IC50 = 2440 nM
|
|
|
| 2 |
Ki = 16 nM
|
|
|
|
CP0542227
|
US9206173, 2409
Show/Hide
|
C27H24ClF3N4O2
|
2
|
| 1 |
IC50 = 2440 nM
|
|
|
| 2 |
Ki = 16 nM
|
|
|
|
CP0414276
|
US9206173, 2446
Show/Hide
|
C30H26F3N5O2
|
2
|
| 1 |
IC50 = 2794 nM
|
|
|
| 2 |
Ki = 28 nM
|
|
|
|
CP0463208
|
US9206173, 2449
Show/Hide
|
C30H26F3N5O2
|
2
|
| 1 |
IC50 = 3350 nM
|
|
|
| 2 |
Ki = 24 nM
|
|
|
|
CP0850664
|
6-[2-(4-chlorophenoxy)acetyl]-2-[(S)-1-(4-chlorophenyl)ethylamino]-3-dimethylamino-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C25H27Cl2N5O3
|
2
|
| 1 |
IC50 = 3600 nM
|
|
|
| 2 |
Ki = 207 nM
|
|
|
|
CP0512666
|
US9206173, 2431
Show/Hide
|
C24H26Cl2N6O3
|
2
|
| 1 |
IC50 = 3600 nM
|
|
|
| 2 |
Ki = 207 nM
|
|
|
|
CP0850660
|
(S)-6-(4-chlorobenzoyl)-3-ethoxy-2-(1-(4-(trifluoromethyl)phenyl)ethylamino)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one
Show/Hide
|
C25H24ClF3N4O3
|
2
|
| 1 |
IC50 = 3710 nM
|
|
|
| 2 |
Ki = 25 nM
|
|
|
|
CP0414283
|
US9206173, 86
Show/Hide
|
C25H24ClF3N4O3
|
2
|
| 1 |
IC50 = 3710 nM
|
|
|
| 2 |
Ki = 25 nM
|
|
|
|
CP0953468
|
6-[3-(4-chlorophenyl)propionyl]-3-methoxy-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C26H26ClF3N4O3
|
2
|
| 1 |
IC50 = 3896 nM
|
|
|
| 2 |
Ki = 134 nM
|
|
|
|
CP0412642
|
US9206173, 2391
Show/Hide
|
C26H26ClF3N4O3
|
2
|
| 1 |
IC50 = 3896 nM
|
|
|
| 2 |
Ki = 134 nM
|
|
|
|
CP0474705
|
US9206173, 2441
Show/Hide
|
C25H26Cl2N4O3
|
2
|
| 1 |
IC50 = 4494 nM
|
|
|
| 2 |
Ki = 37 nM
|
|
|
|
CP0849091
|
6-[(E)-3-(4-chlorophenyl)acryloyl]-3-methoxy-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C26H24ClF3N4O3
|
2
|
| 1 |
IC50 = 5793 nM
|
|
|
| 2 |
Ki = 12 nM
|
|
|
|
CP0512081
|
US9206173, 2392
Show/Hide
|
C25H23ClF3N5O3
|
2
|
| 1 |
IC50 = 5793 nM
|
|
|
| 2 |
Ki = 12 nM
|
|
|
|
CP0849092
|
6-(5-chlorothiophene-2-carbonyl)-3-methoxy-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C22H20ClF3N4O3S
|
2
|
| 1 |
IC50 = 8793 nM
|
|
|
| 2 |
Ki = 15 nM
|
|
|
|
CP0523933
|
US9206173, 2405
Show/Hide
|
C22H20ClF3N4O3S
|
2
|
| 1 |
IC50 = 8793 nM
|
|
|
| 2 |
Ki = 15 nM
|
|
|
|
CP0946609
|
2-[(S)-1-(4-chlorophenyl)ethylamino]-3-methoxy-6-(thieno[2,3-b]pyridine-2-carbonyl)-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one hydrochloride
Show/Hide
|
C24H23Cl2N5O3S
|
1
|
| 1 |
Ki = 3 nM
|
|
|
|
CP0567359
|
US9206173, 2495
Show/Hide
|
C24H22ClN5O3S
|
1
|
| 1 |
Ki = 3 nM
|
|
|
|
CP0426262
|
US9206173, 2456
Show/Hide
|
C26H25F3N4O3
|
1
|
| 1 |
Ki = 6 nM
|
|
|
|
CP0880930
|
4-(2-(3-methoxy-4-oxo-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-3,5,7,8-tetrahydro-4H-pyrido[4,3-d]pyrimidin-6-yl)-2-oxo-ethoxy)benzonitrile
Show/Hide
|
C26H24F3N5O4
|
1
|
| 1 |
Ki = 6 nM
|
|
|
|
CP0561344
|
US9206173, 2468
Show/Hide
|
C26H24F3N5O4
|
1
|
| 1 |
Ki = 6 nM
|
|
|
|
CP0850606
|
6-(3-fluoro-4-methylbenzoyl)-3-methoxy-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C25H24F4N4O3
|
1
|
| 1 |
Ki = 8 nM
|
|
|
|
CP0911812
|
3-fluoro-4-{3-methoxy-4-oxo-2-[(S)-1-(4-trifluoromethylphenyl)propylamino]-3,5,7,8-tetrahydro-4H-pyrido[4,3-d]pyrimidine-6-carbonyl}benzonitrile
Show/Hide
|
C26H23F4N5O3
|
1
|
| 1 |
Ki = 8 nM
|
|
|
|
CP0414280
|
US9206173, 2482
Show/Hide
|
C26H23F4N5O3
|
1
|
| 1 |
Ki = 8 nM
|
|
|
|
CP0527356
|
US9206173, 2457
Show/Hide
|
C25H24F4N4O3
|
1
|
| 1 |
Ki = 8 nM
|
|
|
|
CP0385429
|
US9206173, 2434
Show/Hide
|
C30H27F3N6O2
|
1
|
| 1 |
Ki = 9 nM
|
|
|
|
CP0891840
|
3-{4-oxo-3-(2-propynyl)-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-3,5,7,8-tetrahydro-4H-pyrido[4,3-d]pyrimidine-6-carbonyl}benzonitrile
Show/Hide
|
C27H22F3N5O2
|
1
|
| 1 |
Ki = 9 nM
|
|
|
|
CP0946610
|
3-methoxy-6-(thieno[2,3-b]pyridine-2-carbonyl)-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C25H22F3N5O3S
|
1
|
| 1 |
Ki = 9 nM
|
|
|
|
CP0959625
|
6-(2,6-difluorobenzoyl)-3-(2-propynyl)-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C26H21F5N4O2
|
1
|
| 1 |
Ki = 9 nM
|
|
|
|
CP0557001
|
US9206173, 2476
Show/Hide
|
C26H21F3N6O2
|
1
|
| 1 |
Ki = 9 nM
|
|
|
|
CP0563228
|
US9206173, 2415
Show/Hide
|
C25H22F3N5O3S
|
1
|
| 1 |
Ki = 9 nM
|
|
|
|
CP0566310
|
US9206173, 2478
Show/Hide
|
C25H20F5N5O2
|
1
|
| 1 |
Ki = 9 nM
|
|
|
|
CP0850605
|
6-(2,3-dihydrobenzo[1,4]dioxine-6-carbonyl)-3-methoxy-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C26H25F3N4O5
|
1
|
| 1 |
Ki = 10 nM
|
|
|
|
CP0948122
|
3-methoxy-6-(4-methyl-4H-furo[3,2-b]pyrrole-5-carbonyl)-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C25H24F3N5O4
|
1
|
| 1 |
Ki = 10 nM
|
|
|
|
CP0542223
|
US9206173, 2459
Show/Hide
|
C26H25F3N4O5
|
1
|
| 1 |
Ki = 10 nM
|
|
|
|
CP0571496
|
US9206173, 2465
Show/Hide
|
C25H24F3N5O4
|
1
|
| 1 |
Ki = 10 nM
|
|
|
|
CP0891838
|
2-[(S)-1-(4-chlorophenyl)-2-methylpropylamino]-3-methoxy-6-(pyrazolo[1,5-a]pyridine-2-carbonyl)-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C26H27ClN6O3
|
1
|
| 1 |
Ki = 13 nM
|
|
|
|
CP0561345
|
US9206173, 2483
Show/Hide
|
C26H27ClN6O3
|
1
|
| 1 |
Ki = 13 nM
|
|
|
|
CP0963534
|
3-methoxy-6-(5-methoxybenzofuran-2-carbonyl)-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C27H25F3N4O5
|
1
|
| 1 |
Ki = 14 nM
|
|
|
|
CP0559721
|
US9206173, 2460
Show/Hide
|
C27H25F3N4O5
|
1
|
| 1 |
Ki = 14 nM
|
|
|
|
CP0963535
|
6-(benzo[b]thiophene-2-carbonyl)-3-methoxy-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C26H25F3N4O3S
|
1
|
| 1 |
Ki = 15 nM
|
|
|
|
CP0414278
|
US9206173, 2474
Show/Hide
|
C26H23F3N4O3S
|
1
|
| 1 |
Ki = 15 nM
|
|
|
|
CP0911810
|
3-methoxy-6-(1-methyl-2-oxo-1,2,3,4-tetrahydro-quinoline-6-carbonyl)-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C28H28F3N5O4
|
1
|
| 1 |
Ki = 16 nM
|
|
|
|
CP0559722
|
US9206173, 2461
Show/Hide
|
C28H28F3N5O4
|
1
|
| 1 |
Ki = 16 nM
|
|
|
|
CP0877214
|
6-(4-chloro-2-methoxybenzoyl)-3-methoxy-2-[(S)-1-(4-trifluoromethylphenyl)ethylaminol-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C25H24ClF3N4O4
|
1
|
| 1 |
Ki = 18 nM
|
|
|
|
CP0512665
|
US9206173, 2414
Show/Hide
|
C25H24ClF3N4O4
|
1
|
| 1 |
Ki = 18 nM
|
|
|
|
CP0968300
|
3-methoxy-6-(1-methyl-5-thiophen-2-yl-1H-pyrazole-3-carbonyl)-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C26H25F3N6O3S
|
1
|
| 1 |
Ki = 20 nM
|
|
|
|
CP0518619
|
US9206173, 2464
Show/Hide
|
C26H25F3N6O3S
|
1
|
| 1 |
Ki = 20 nM
|
|
|
|
CP0559719
|
US9206173, 2448
Show/Hide
|
C28H27F3N4O3
|
1
|
| 1 |
Ki = 23 nM
|
|
|
|
CP0902282
|
2-[(S)-1-(4-chlorophenyl)-2-methylpropylamino]-3-methoxy-6-(1-methyl-2-oxo-1,2,3,4-tetrahydro-quinoline-6-carbonyl)-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C29H32ClN5O4
|
1
|
| 1 |
Ki = 24 nM
|
|
|
|
CP0561346
|
US9206173, 2487
Show/Hide
|
C29H32ClN5O4
|
1
|
| 1 |
Ki = 24 nM
|
|
|
|
CP0556999
|
US9206173, 2438
Show/Hide
|
C30H26F3N5O3
|
1
|
| 1 |
Ki = 26 nM
|
|
|
|
CP0894649
|
2-[(S)-1-(4-chlorophenyl)-2-methylpropylamino]-6-(isoquinoline-3-carbonyl)-3-methoxy-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C28H28ClN5O3
|
1
|
| 1 |
Ki = 26 nM
|
|
|
|
CP0567358
|
US9206173, 2489
Show/Hide
|
C28H28ClN5O3
|
1
|
| 1 |
Ki = 26 nM
|
|
|
|
CP0891839
|
2-[(S)-1-(4-chlorophenyl)-2-methylpropylamino]-6-(4-imidazol-1-ylbenzoyl)-3-methoxy-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C28H29ClN6O3
|
1
|
| 1 |
Ki = 31 nM
|
|
|
|
CP0567098
|
US9206173, 2481
Show/Hide
|
C28H29ClN6O3
|
1
|
| 1 |
Ki = 31 nM
|
|
|
|
CP0954143
|
3-fluoro-4-(3-isobutoxy-4-oxo-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-3,5,7,8-tetrahydro-4H-pyrido[4,3-d]pyrimidine-6-carbonyl}benzonitrile
Show/Hide
|
C28H27F4N5O3
|
1
|
| 1 |
Ki = 33 nM
|
|
|
|
CP0414273
|
US9206173, 2416
Show/Hide
|
C28H27F4N5O3
|
1
|
| 1 |
Ki = 33 nM
|
|
|
|
CP0518621
|
US9206173, 2475
Show/Hide
|
C26H24ClF3N4O3
|
1
|
| 1 |
Ki = 34 nM
|
|
|
|
CP0896786
|
6-(4-chlorobenzoyl)-3-methoxy-2-(4-trifluoromethylbenzylamino)-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one hydrochloride
Show/Hide
|
C23H21Cl2F3N4O3
|
1
|
| 1 |
Ki = 39 nM
|
|
|
|
CP0567097
|
US9206173, 2477
Show/Hide
|
C23H20ClF3N4O3
|
1
|
| 1 |
Ki = 39 nM
|
|
|
|
CP0571495
|
US9206173, 2447
Show/Hide
|
C29H29F3N4O2
|
1
|
| 1 |
Ki = 41 nM
|
|
|
|
CP0954142
|
3-(3-butynyl)-6-(4-methylbenzoyl)-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C28H27F3N4O2
|
1
|
| 1 |
Ki = 41 nM
|
|
|
|
CP0571494
|
US9206173, 2443
Show/Hide
|
C27H26F3N5O2
|
1
|
| 1 |
Ki = 41 nM
|
|
|
|
CP0414275
|
US9206173, 2444
Show/Hide
|
C28H25F3N4O4
|
1
|
| 1 |
Ki = 42 nM
|
|
|
|
CP0904422
|
2-[(S)-1-(4-chlorophenyl)-2-methylpropylamino]-6-(2,3-dihydrobenzo[1,4]dioxine-6-carbonyl)-3-methoxy-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C27H29ClN4O5
|
1
|
| 1 |
Ki = 42 nM
|
|
|
|
CP0523930
|
US9206173, 2479
Show/Hide
|
C27H29ClN4O5
|
1
|
| 1 |
Ki = 42 nM
|
|
|
|
CP0963533
|
6-(5-chloro-furan-2-carbonyl)-3-methoxy-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C22H20ClF3N4O4
|
1
|
| 1 |
Ki = 48 nM
|
|
|
|
CP0542222
|
US9206173, 2454
Show/Hide
|
C22H20ClF3N4O4
|
1
|
| 1 |
Ki = 48 nM
|
|
|
|
CP0952765
|
4-[2-((S)-1-cyclohexylethylamino)-3-methoxy-4-oxo-3,5,7,8-tetrahydro-4H-pyrido[4,3-d]pyrimidine-6-carbonyl]-3-fluorobenzonitrile
Show/Hide
|
C24H28FN5O3
|
1
|
| 1 |
Ki = 56 nM
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|
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CP0518620
|
US9206173, 2469
Show/Hide
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C24H28FN5O3
|
1
|
| 1 |
Ki = 56 nM
|
|
|
|
CP0952764
|
4-[2-((R)-1-cyclohexyl-ethylamino)-3-methoxy-4-oxo-3,5,7,8-tetrahydro-4H-pyrido[4,3-d]pyrimidine-6-carbonyl]-3-fluorobenzonitrile
Show/Hide
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C24H28FN5O3
|
1
|
| 1 |
Ki = 61 nM
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|
|
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CP0559723
|
US9206173, 2472
Show/Hide
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C25H29FN4O3
|
1
|
| 1 |
Ki = 61 nM
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|
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CP0880931
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6-(4-chlorobenzoyl)-2-(4-chlorobenzylamino)-3-methoxy-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one hydrochloride
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|
C22H21Cl3N4O3
|
1
|
| 1 |
Ki = 98 nM
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|
|
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CP0567357
|
US9206173, 2462
Show/Hide
|
C22H20Cl2N4O3
|
1
|
| 1 |
Ki = 98 nM
|
|
|
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CP0896785
|
6-(4-chlorobenzoyl)-2-((S)-1-cyclohexyl-ethylamino)-3-methoxy-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C23H29ClN4O3
|
1
|
| 1 |
Ki = 108 nM
|
|
|
|
CP0423842
|
US9206173, 2470
Show/Hide
|
C23H29ClN4O3
|
1
|
| 1 |
Ki = 108 nM
|
|
|
|
CP0559720
|
US9206173, 2450
Show/Hide
|
C25H23Cl2F3N4O3
|
1
|
| 1 |
Ki = 121 nM
|
|
|
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CP0863157
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6-[2-(4-chlorophenoxy)acetyl]-3-dimethylamino-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one hydrochloride
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|
C26H28Cl2F3N5O3
|
1
|
| 1 |
Ki = 140 nM
|
|
|
|
CP0519920
|
US9206173, 2442
Show/Hide
|
C25H26ClF3N6O3
|
1
|
| 1 |
Ki = 140 nM
|
|
|
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CP0456489
|
US9206173, 2494
Show/Hide
|
C30H30F3N5O3
|
1
|
| 1 |
Ki = 201 nM
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|
|
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CP0487170
|
US9206173, 2490
Show/Hide
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C25H24FN5O4
|
1
|
| 1 |
Ki = 237 nM
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|
|
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CP0910409
|
6-(1H-benzoimidazole-2-carbonyl)-3-(3-butynyl)-2-[(S)-1-(4-trifluoromethylphenyl)ethylamino]-5,6,7,8-tetrahydro-3H-pyrido[4,3-d]pyrimidin-4-one
Show/Hide
|
C28H25F3N6O2
|
1
|
| 1 |
Ki = 245 nM
|
|
|
