Brief Information of the Cell Line and Protein
Cell Line ID: CL000128 , TF-1
Synonyms
TF1
MFD-1
Category Cancer cell line
Organism
Homo sapiens (Human)
Cellosaurus ID
CVCL_0559
Protein ID: PT01659 , Tyrosine-protein kinase JAK1
Gene Name JAK1
Organism Homo sapiens, Human
Protein Classification Kinase
Uniprot ID P23458
Table of Molecular Bioactivities Related to the Cell Line and Protein
Cell Line ID: CL000128  Protein ID: PT01659
 
Compound ID Compound Name Compound Formula
CP0108652
2-[4-[4-[(1R)-1-hydroxyethyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]cyclohexyl]acetonitrile
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C18H21N5O
 2
1
EC50 = 5.7 nM
   TI
   LI
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   TS
2
EC50 = 28 nM
   TI
   LI
   LO
   TS
CP0088219
N-[[3-[(1R,2R,4S)-2-bicyclo[2.2.1]heptanyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]methanesulfonamide
   Show/Hide
C17H21N5O2S
 2
1
EC50 = 13 nM
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2
EC50 = 118 nM
   TI
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   TS
CP0012129
INCB-018424
   Show/Hide
C17H18N6
 1
1
EC50 = 24 nM
   TI
   LI
   LO
   TS
CP0255798
3-[4-(4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]propanenitrile
   Show/Hide
C17H20N6
 1
1
EC50 = 26 nM
   TI
   LI
   LO
   TS
CP0084964
(1R)-1-[3-[4-(2,2,2-trifluoroethylamino)cyclohexyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]ethanol
   Show/Hide
C18H22F3N5O
 2
1
EC50 = 28 nM
   TI
   LI
   LO
   TS
2
EC50 = 29 nM
   TI
   LI
   LO
   TS
CP0087139
3-[4-[4-[(1R)-1-hydroxyethyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]cyclohexyl]propanenitrile
   Show/Hide
C19H23N5O
 2
1
EC50 = 33 nM
   TI
   LI
   LO
   TS
2
EC50 = 43 nM
   TI
   LI
   LO
   TS
CP0260731
3-(1-benzylpiperidin-4-yl)-4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene
   Show/Hide
C21H23N5
 1
1
EC50 = 35 nM
   TI
   LI
   LO
   TS
CP0079525
3-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]propanenitrile
   Show/Hide
C16H18N6
 1
1
EC50 = 43 nM
   TI
   LI
   LO
   TS
CP0002393
3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile
   Show/Hide
C16H20N6O
 2
1
EC50 = 43 nM
   TI
   LI
   LO
   TS
2
EC50 = 53 nM
   TI
   LI
   LO
   TS
CP0266379
(1R)-1-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)ethanol
   Show/Hide
C16H20N4O
 2
1
EC50 = 47 nM
   TI
   LI
   LO
   TS
2
EC50 = 330 nM
   TI
   LI
   LO
   TS
CP0261449
4-[4-[(1R)-1-hydroxyethyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]cyclohexane-1-carbonitrile
   Show/Hide
C17H19N5O
 2
1
EC50 = 49 nM
   TI
   LI
   LO
   TS
2
EC50 = 78 nM
   TI
   LI
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   TS
CP0329529
N-[2-[3-(2-bicyclo[2.2.1]heptanyl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]ethyl]methanesulfonamide
   Show/Hide
C18H23N5O2S
 1
1
EC50 = 50 nM
   TI
   LI
   LO
   TS
CP0087579
(1R)-1-[3-[(1S,3R)-3-(2,2,2-trifluoroethylamino)cyclopentyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]ethanol
   Show/Hide
C17H20F3N5O
 2
1
EC50 = 51 nM
   TI
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   TS
2
EC50 = 70 nM
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   TS
CP0315771
3-[(3R,4R)-3-fluoropiperidin-4-yl]-4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene
   Show/Hide
C14H16FN5
 1
1
EC50 = 57 nM
   TI
   LI
   LO
   TS
CP0265330
(1R)-1-[3-[4-(2,2-difluoroethylamino)cyclohexyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]ethanol
   Show/Hide
C18H23F2N5O
 2
1
EC50 = 57 nM
   TI
   LI
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   TS
2
EC50 = 62 nM
   TI
   LI
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   TS
CP0084967
(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)methanol
   Show/Hide
C15H18N4O
 2
1
EC50 = 64 nM
   TI
   LI
   LO
   TS
2
EC50 = 313 nM
   TI
   LI
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   TS
CP0369955
(1S)-1-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)ethane-1,2-diol
   Show/Hide
C16H20N4O2
 2
1
EC50 = 69 nM
   TI
   LI
   LO
   TS
2
EC50 = 220 nM
   TI
   LI
   LO
   TS
CP0285868
(1R)-1-[3-[(1S,3S)-3-(2,2,2-trifluoroethylamino)cyclopentyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]ethanol
   Show/Hide
C17H20F3N5O
 2
1
EC50 = 74 nM
   TI
   LI
   LO
   TS
2
EC50 = 82 nM
   TI
   LI
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   TS
CP0359333
(1R)-1-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)propan-1-ol
   Show/Hide
C17H22N4O
 2
1
EC50 = 84 nM
   TI
   LI
   LO
   TS
2
EC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0247748
3-(1-benzylpiperidin-4-yl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene
   Show/Hide
C20H21N5
 1
1
EC50 = 86 nM
   TI
   LI
   LO
   TS
CP0120553
(1R,3R)-3-(4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexan-1-ol
   Show/Hide
C15H18N4O
 2
1
EC50 = 87 nM
   TI
   LI
   LO
   TS
2
EC50 = 160 nM
   TI
   LI
   LO
   TS
CP0261451
(1R)-1-[3-(1-ethyl-3,3-difluoropiperidin-4-yl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]ethanol
   Show/Hide
C17H21F2N5O
 2
1
EC50 = 88 nM
   TI
   LI
   LO
   TS
2
EC50 = 330 nM
   TI
   LI
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   TS
CP0146865
3-cyclohexyl-4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene
   Show/Hide
C15H18N4
 2
1
EC50 = 100 nM
   TI
   LI
   LO
   TS
2
EC50 = 180 nM
   TI
   LI
   LO
   TS
CP0178056
3-[[4-(4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexyl]amino]propanenitrile
   Show/Hide
C18H22N6
 1
1
EC50 = 110 nM
   TI
   LI
   LO
   TS
CP0108487
(1R)-1-[3-[(3S)-oxan-3-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]ethanol
   Show/Hide
C15H18N4O2
 2
1
EC50 = 110 nM
   TI
   LI
   LO
   TS
2
EC50 = 180 nM
   TI
   LI
   LO
   TS
CP0266378
(1R)-1-[3-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]ethanol
   Show/Hide
C17H20F3N5O
 2
1
EC50 = 110 nM
   TI
   LI
   LO
   TS
2
EC50 = 820 nM
   TI
   LI
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   TS
CP0108702
3-oxo-3-[(3R)-3-(3,4,5,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1,5,7,9,11-pentaen-3-yl)piperidin-1-yl]propanenitrile
   Show/Hide
C15H15N7O
 1
1
EC50 = 114 nM
   TI
   LI
   LO
   TS
CP0102822
4-[4-[(1R)-1-hydroxyethyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]cyclohexane-1-carbonitrile
   Show/Hide
C17H19N5O
 2
1
EC50 = 120 nM
   TI
   LI
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   TS
2
EC50 = 130 nM
   TI
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   TS
CP0198952
(1R,3R)-3-[4-[(1R)-1-hydroxyethyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]cyclohexan-1-ol
   Show/Hide
C16H20N4O2
 2
1
EC50 = 120 nM
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   LI
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   TS
2
EC50 = 140 nM
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CP0217586
CHEMBL2392487
   Show/Hide
C19H20N6
 1
1
EC50 = 121 nM
   TI
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   LO
   TS
CP0104959
tert-butyl N-[(1R,3R)-3-(3,4,5,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1,5,7,9,11-pentaen-3-yl)cyclopentyl]carbamate
   Show/Hide
C17H22N6O2
 1
1
EC50 = 127 nM
   TI
   LI
   LO
   TS
CP0257219
N-(cyclopropylmethyl)-4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexan-1-amine
   Show/Hide
C18H23N5
 1
1
EC50 = 130 nM
   TI
   LI
   LO
   TS
CP0329462
N-[(3-cycloheptyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)methyl]methanesulfonamide
   Show/Hide
C17H23N5O2S
 1
1
EC50 = 130 nM
   TI
   LI
   LO
   TS
CP0266430
2-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)ethanol
   Show/Hide
C16H20N4O
 2
1
EC50 = 130 nM
   TI
   LI
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   TS
2
EC50 = 1500 nM
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   TS
CP0086382
3-[4-(3,4,5,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1,5,7,9,11-pentaen-3-yl)piperidin-1-yl]propanenitrile
   Show/Hide
C15H17N7
 1
1
EC50 = 138 nM
   TI
   LI
   LO
   TS
CP0355897
3-(1-methylsulfonylpiperidin-4-yl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene
   Show/Hide
C14H17N5O2S
 1
1
EC50 = 140 nM
   TI
   LI
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   TS
CP0179649
methyl N-[(1R,3R)-3-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclopentyl]carbamate
   Show/Hide
C15H17N5O2
 1
1
EC50 = 150 nM
   TI
   LI
   LO
   TS
CP0130638
12-cyclohexyl-1,5,7,10-tetrazatricyclo[7.3.0.02,6]dodeca-2(6),3,7,9,11-pentaene
   Show/Hide
C14H16N4
 1
1
EC50 = 150 nM
   TI
   LI
   LO
   TS
CP0335391
3-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene
   Show/Hide
C15H16F3N5
 1
1
EC50 = 160 nM
   TI
   LI
   LO
   TS
CP0120790
N-[[3-[(1S,2S,4R)-2-bicyclo[2.2.1]heptanyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]methanesulfonamide
   Show/Hide
C17H21N5O2S
 1
1
EC50 = 160 nM
   TI
   LI
   LO
   TS
CP0175649
3-[4-(4-cyclopropyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]propanenitrile
   Show/Hide
C19H22N6
 1
1
EC50 = 160 nM
   TI
   LI
   LO
   TS
CP0204289
N-[[3-(2-bicyclo[2.2.1]heptanyl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]acetamide
   Show/Hide
C18H21N5O
 1
1
EC50 = 160 nM
   TI
   LI
   LO
   TS
CP0086377
3-[[4-(3,4,5,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1,5,7,9,11-pentaen-3-yl)cyclohexyl]amino]propanenitrile
   Show/Hide
C16H19N7
 1
1
EC50 = 165 nM
   TI
   LI
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   TS
CP0146867
3-cyclohexyl-4,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1(12),2,6,8,10-pentaene
   Show/Hide
C14H16N4
 1
1
EC50 = 170 nM
   TI
   LI
   LO
   TS
CP0186393
3-oxo-3-[(3R)-3-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]propanenitrile
   Show/Hide
C16H16N6O
 1
1
EC50 = 180 nM
   TI
   LI
   LO
   TS
CP0270172
3-[[[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexyl]amino]methyl]benzonitrile
   Show/Hide
C22H22N6
 1
1
EC50 = 180 nM
   TI
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   TS
CP0335392
tert-butyl N-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexyl]carbamate
   Show/Hide
C19H25N5O2
 1
1
EC50 = 180 nM
   TI
   LI
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   TS
CP0356714
4-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexyl]morpholine
   Show/Hide
C18H23N5O
 1
1
EC50 = 180 nM
   TI
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   TS
CP0120685
(1R,3R)-3-(4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclopentan-1-ol
   Show/Hide
C14H16N4O
 1
1
EC50 = 180 nM
   TI
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   TS
CP0171798
N-[2-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)ethyl]methanesulfonamide
   Show/Hide
C17H23N5O2S
 1
1
EC50 = 180 nM
   TI
   LI
   LO
   TS
CP0120684
(1R,3S)-3-(4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclopentan-1-ol
   Show/Hide
C14H16N4O
 1
1
EC50 = 190 nM
   TI
   LI
   LO
   TS
CP0088169
N-[(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)methyl]methanesulfonamide
   Show/Hide
C16H21N5O2S
 1
1
EC50 = 190 nM
   TI
   LI
   LO
   TS
CP0255709
3-(4-methyl-1-methylsulfonylpiperidin-4-yl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene
   Show/Hide
C15H19N5O2S
 1
1
EC50 = 210 nM
   TI
   LI
   LO
   TS
CP0323372
N-[2-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)ethyl]acetamide
   Show/Hide
C18H23N5O
 1
1
EC50 = 210 nM
   TI
   LI
   LO
   TS
CP0168169
1-cyclohexyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine (2)
   Show/Hide
C14H16N4
 1
1
EC50 = 210 nM
   TI
   LI
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   TS
CP0305359
3-(4-methyl-1-methylsulfonylpiperidin-4-yl)-3,4,5,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1,5,7,9,11-pentaene
   Show/Hide
C14H18N6O2S
 1
1
EC50 = 220 nM
   TI
   LI
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   TS
CP0107727
CHEMBL2386628
   Show/Hide
C17H22N4O2
 2
1
EC50 = 240 nM
   TI
   LI
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2
EC50 = 280 nM
   TI
   LI
   LO
   TS
CP0086379
3-(1-methylsulfonylpiperidin-4-yl)-3,4,5,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1,5,7,9,11-pentaene
   Show/Hide
C13H16N6O2S
 1
1
EC50 = 249 nM
   TI
   LI
   LO
   TS
CP0100650
4-methyl-3-piperidin-4-yl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene
   Show/Hide
C14H17N5
 1
1
EC50 = 250 nM
   TI
   LI
   LO
   TS
CP0161562
4-(4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexan-1-ol
   Show/Hide
C15H18N4O
 1
1
EC50 = 250 nM
   TI
   LI
   LO
   TS
CP0334376
4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexan-1-amine
   Show/Hide
C14H17N5
 1
1
EC50 = 260 nM
   TI
   LI
   LO
   TS
CP0302958
tert-butyl N-[(1S,3R)-3-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclopentyl]carbamate
   Show/Hide
C18H23N5O2
 1
1
EC50 = 270 nM
   TI
   LI
   LO
   TS
CP0178017
4-(4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexan-1-ol
   Show/Hide
C15H18N4O
 1
1
EC50 = 270 nM
   TI
   LI
   LO
   TS
CP0334795
3-[4-(4-propyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]propanenitrile
   Show/Hide
C19H24N6
 1
1
EC50 = 275 nM
   TI
   LI
   LO
   TS
CP0159699
CHEMBL2159208
   Show/Hide
C17H21N5O2
 1
1
EC50 = 280 nM
   TI
   LI
   LO
   TS
CP0315684
(1R,3S)-3-(4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexan-1-ol
   Show/Hide
C15H18N4O
 1
1
EC50 = 310 nM
   TI
   LI
   LO
   TS
CP0369957
3-[4-[4-[(1R)-1-hydroxyethyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]piperidin-1-yl]propanenitrile
   Show/Hide
C18H22N6O
 2
1
EC50 = 320 nM
   TI
   LI
   LO
   TS
2
EC50 = 510 nM
   TI
   LI
   LO
   TS
CP0285853
(1R)-1-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)ethane-1,2-diol
   Show/Hide
C16H20N4O2
 1
1
EC50 = 320 nM
   TI
   LI
   LO
   TS
CP0088171
N-[[3-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]methanesulfonamide
   Show/Hide
C17H21F3N6O2S
 1
1
EC50 = 325 nM
   TI
   LI
   LO
   TS
CP0100646
2-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)propan-2-ol
   Show/Hide
C17H22N4O
 1
1
EC50 = 330 nM
   TI
   LI
   LO
   TS
CP0340065
4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexan-1-amine
   Show/Hide
C14H17N5
 1
1
EC50 = 340 nM
   TI
   LI
   LO
   TS
CP0339507
3-[1-(pyrimidin-5-ylmethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene
   Show/Hide
C18H19N7
 1
1
EC50 = 350 nM
   TI
   LI
   LO
   TS
CP0142992
4-methyl-3-[(3S)-oxan-3-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene
   Show/Hide
C14H16N4O
 1
1
EC50 = 350 nM
   TI
   LI
   LO
   TS
CP0315770
3-(3,3-difluoropiperidin-4-yl)-4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene
   Show/Hide
C14H15F2N5
 1
1
EC50 = 350 nM
   TI
   LI
   LO
   TS
CP0108248
12-cyclohexyl-1,5,7,10,11-pentazatricyclo[7.3.0.02,6]dodeca-2(6),3,7,9,11-pentaene
   Show/Hide
C13H15N5
 1
1
EC50 = 350 nM
   TI
   LI
   LO
   TS
CP0086380
3-methyl-N-[4-(3,4,5,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1,5,7,9,11-pentaen-3-yl)cyclohexyl]butanamide
   Show/Hide
C18H24N6O
 1
1
EC50 = 350 nM
   TI
   LI
   LO
   TS
CP0107726
(1S)-1-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)ethanol
   Show/Hide
C16H20N4O
 1
1
EC50 = 360 nM
   TI
   LI
   LO
   TS
CP0146866
12-cyclohexyl-1,5,7,11-tetrazatricyclo[7.3.0.02,6]dodeca-2(6),3,7,9,11-pentaene
   Show/Hide
C14H16N4
 1
1
EC50 = 370 nM
   TI
   LI
   LO
   TS
CP0369956
CHEMBL2386626
   Show/Hide
C16H20N4O2
 1
1
EC50 = 380 nM
   TI
   LI
   LO
   TS
CP0087922
methyl N-[(1R,3R)-3-(3,4,5,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1,5,7,9,11-pentaen-3-yl)cyclopentyl]carbamate
   Show/Hide
C14H16N6O2
 1
1
EC50 = 395 nM
   TI
   LI
   LO
   TS
CP0508197
methyl N-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexyl]carbamate
   Show/Hide
C16H19N5O2
 1
1
EC50 = 400 nM
   TI
   LI
   LO
   TS
CP0334377
2-methyl-N-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexyl]propanamide
   Show/Hide
C18H23N5O
 1
1
EC50 = 410 nM
   TI
   LI
   LO
   TS
CP0310453
3-[4-(4-propan-2-yl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]propanenitrile
   Show/Hide
C19H24N6
 1
1
EC50 = 410 nM
   TI
   LI
   LO
   TS
CP0112715
(1S)-1-(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)propan-1-ol
   Show/Hide
C17H22N4O
 1
1
EC50 = 410 nM
   TI
   LI
   LO
   TS
CP0261450
4-[4-[(1R)-1-hydroxyethyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]cyclohexan-1-ol
   Show/Hide
C16H20N4O2
 2
1
EC50 = 410 nM
   TI
   LI
   LO
   TS
2
EC50 = 730 nM
   TI
   LI
   LO
   TS
CP0157841
CHEMBL2392490
   Show/Hide
C18H19N7
 1
1
EC50 = 414 nM
   TI
   LI
   LO
   TS
CP0426744
3-[4-(4-cyclobutyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]propanenitrile
   Show/Hide
C20H24N6
 1
1
EC50 = 430 nM
   TI
   LI
   LO
   TS
CP0130641
3-cyclohexyl-5-oxa-4,8,10-triazatricyclo[7.3.0.02,6]dodeca-1(12),2,6,8,10-pentaene
   Show/Hide
C14H15N3O
 1
1
EC50 = 430 nM
   TI
   LI
   LO
   TS
CP0104957
methyl N-[4-(3,4,5,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1,5,7,9,11-pentaen-3-yl)cyclohexyl]carbamate
   Show/Hide
C15H18N6O2
 1
1
EC50 = 433 nM
   TI
   LI
   LO
   TS
CP0359605
3-[[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexyl]amino]propanenitrile
   Show/Hide
C17H20N6
 1
1
EC50 = 440 nM
   TI
   LI
   LO
   TS
CP0178020
3-[(3S,4R)-3-fluoropiperidin-4-yl]-4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene
   Show/Hide
C14H16FN5
 1
1
EC50 = 490 nM
   TI
   LI
   LO
   TS
CP0079526
tert-butyl N-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexyl]carbamate
   Show/Hide
C19H25N5O2
 1
1
EC50 = 500 nM
   TI
   LI
   LO
   TS
CP0321389
3-(1-ethylpiperidin-4-yl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene
   Show/Hide
C15H19N5
 1
1
EC50 = 520 nM
   TI
   LI
   LO
   TS
CP0165766
3-[1-(benzenesulfonyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene
   Show/Hide
C19H19N5O2S
 1
1
EC50 = 540 nM
   TI
   LI
   LO
   TS
CP0339771
4-(3,4,5,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1,5,7,9,11-pentaen-3-yl)cyclohexan-1-ol
   Show/Hide
C13H15N5O
 1
1
EC50 = 558 nM
   TI
   LI
   LO
   TS
CP0247830
3-[4-[4-[2-(oxolan-2-yl)ethyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]piperidin-1-yl]propanenitrile
   Show/Hide
C22H28N6O
 1
1
EC50 = 570 nM
   TI
   LI
   LO
   TS
CP0369176
ethyl N-[[3-[1-(2-cyanoethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]carbamate
   Show/Hide
C20H25N7O2
 1
1
EC50 = 625 nM
   TI
   LI
   LO
   TS
CP0186394
3-[4-methyl-1-(pyrimidin-5-ylmethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene
   Show/Hide
C19H21N7
 1
1
EC50 = 670 nM
   TI
   LI
   LO
   TS
CP0194789
methyl N-methyl-N-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexyl]carbamate
   Show/Hide
C17H21N5O2
 1
1
EC50 = 670 nM
   TI
   LI
   LO
   TS
CP0329463
N-[(3-cyclohexyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)methyl]acetamide
   Show/Hide
C17H21N5O
 1
1
EC50 = 670 nM
   TI
   LI
   LO
   TS
CP0356271
N-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexyl]methanesulfonamide
   Show/Hide
C15H19N5O2S
 1
1
EC50 = 700 nM
   TI
   LI
   LO
   TS
CP0217584
4-(3,4,5,8,10-pentazatricyclo[7.3.0.02,6]dodeca-1,5,7,9,11-pentaen-3-yl)cyclohexan-1-amine
   Show/Hide
C13H16N6
 1
1
EC50 = 729 nM
   TI
   LI
   LO
   TS
CP0323371
N-[(3-cyclopentyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl)methyl]methanesulfonamide
   Show/Hide
C15H19N5O2S
 1
1
EC50 = 815 nM
   TI
   LI
   LO
   TS
CP0525615
3-(4-methylpiperidin-4-yl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene
   Show/Hide
C14H17N5
 1
1
EC50 = 880 nM
   TI
   LI
   LO
   TS
CP0178055
N-[4-(4-methyl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexyl]methanesulfonamide
   Show/Hide
C16H21N5O2S
 1
1
EC50 = 890 nM
   TI
   LI
   LO
   TS
CP0146014
3-cyclohexyl-4-(trifluoromethyl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene
   Show/Hide
C15H15F3N4
 1
1
EC50 = 970 nM
   TI
   LI
   LO
   TS
CP0159700
4-methyl-3-(oxan-4-yl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene
   Show/Hide
C14H16N4O
 1
1
EC50 = 990 nM
   TI
   LI
   LO
   TS
CP0323227
N-[[3-[1-(2-cyanoethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]-2-methylpropane-1-sulfonamide
   Show/Hide
C21H29N7O2S
 1
1
EC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0146868
3-cyclohexyl-5-methyl-4,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1(12),2,6,8,10-pentaene
   Show/Hide
C15H18N4
 1
1
EC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0274109
phenyl-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]methanone
   Show/Hide
C20H19N5O
 1
1
EC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0369177
3-[4-[4-(oxolan-2-ylmethyl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]piperidin-1-yl]propanenitrile
   Show/Hide
C21H26N6O
 1
1
EC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0112719
3-piperidin-4-yl-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaene
   Show/Hide
C13H15N5
 1
1
EC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0345484
N-[[3-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]acetamide
   Show/Hide
C18H21F3N6O
 1
1
EC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0186640
[(2S)-1-methylpiperidin-2-yl]-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]methanone
   Show/Hide
C20H26N6O
 1
1
EC50 = 1800 nM
   TI
   LI
   LO
   TS
CP0282470
3-methyl-1-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]butan-1-one
   Show/Hide
C18H23N5O
 1
1
EC50 = 1800 nM
   TI
   LI
   LO
   TS
CP0274441
3-[4-[4-(2-pyrazol-1-ylethyl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]piperidin-1-yl]propanenitrile
   Show/Hide
C21H24N8
 1
1
EC50 = 1800 nM
   TI
   LI
   LO
   TS
CP0076053
3-[4-[4-(cyclopentylmethyl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]piperidin-1-yl]propanenitrile
   Show/Hide
C22H28N6
 1
1
EC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0274272
N-[[3-[(1R,3R)-3-hydroxycyclohexyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]methanesulfonamide
   Show/Hide
C16H21N5O3S
 1
1
EC50 = 2200 nM
   TI
   LI
   LO
   TS
CP0088180
3-[4-[4-(oxan-4-ylmethyl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]piperidin-1-yl]propanenitrile
   Show/Hide
C22H28N6O
 1
1
EC50 = 2600 nM
   TI
   LI
   LO
   TS
CP0106619
3-[4-[4-[2-(1-methylpyrazol-3-yl)ethyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]piperidin-1-yl]propanenitrile
   Show/Hide
C22H26N8
 1
1
EC50 = 2600 nM
   TI
   LI
   LO
   TS
CP0315772
CHEMBL2159207
   Show/Hide
C17H21N5O
 1
1
EC50 = 3600 nM
   TI
   LI
   LO
   TS
CP0284087
N-[[3-(7-oxabicyclo[2.2.1]heptan-2-yl)-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]methanesulfonamide
   Show/Hide
C16H19N5O3S
 1
1
EC50 = 4200 nM
   TI
   LI
   LO
   TS
CP0194788
4-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)cyclohexyl]morpholine
   Show/Hide
C18H23N5O
 1
1
EC50 = 5200 nM
   TI
   LI
   LO
   TS
CP0247820
3-[4-[4-[2-(1-methylimidazol-2-yl)ethyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]piperidin-1-yl]propanenitrile
   Show/Hide
C22H26N8
 1
1
EC50 = 5200 nM
   TI
   LI
   LO
   TS
CP0265331
3-[(3R)-3-[4-[(1R)-1-hydroxyethyl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl]piperidin-1-yl]-3-oxopropanenitrile
   Show/Hide
C18H20N6O2
 1
1
EC50 = 8200 nM
   TI
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CP0079522
3-oxo-3-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]propanenitrile
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C16H16N6O
 1
1
EC50 > 10000 nM
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CP0345485
N-[[3-[1-(2-cyanoethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]methanesulfonamide
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C18H23N7O2S
 1
1
EC50 > 3500 nM
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CP0207474
N-[[3-[1-(2-cyanoethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]methyl]acetamide
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C19H23N7O
 1
1
EC50 > 3800 nM
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CP0270257
N-[2-[3-[1-(2-cyanoethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]ethyl]methanesulfonamide
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C19H25N7O2S
 1
1
EC50 > 6000 nM
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CP0369175
N-[2-[3-[1-(2-cyanoethyl)piperidin-4-yl]-3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-4-yl]ethyl]acetamide
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C20H25N7O
 1
1
EC50 > 6500 nM
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CP0351812
2-(dimethylamino)-1-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]ethanone
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C17H22N6O
 1
1
EC50 > 7100 nM
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CP0257242
[(2S)-1-methylpyrrolidin-2-yl]-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]methanone
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C19H24N6O
 1
1
EC50 > 8600 nM
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CP0355898
[(2S)-1-propan-2-ylpyrrolidin-2-yl]-[4-(3,5,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1,4,6,8,11-pentaen-3-yl)piperidin-1-yl]methanone
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C21H28N6O
 1
1
EC50 > 8800 nM
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CP0644560
4-((cis-1-(4-Chlorobenzyl)-2-methylpiperidin-4-yl)amino)-N-methyl-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
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C22H26ClN5O
 1
1
IC50 = 230 nM
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