General Information of the Protein
Protein ID
PT01491
Protein Name
Metabotropic glutamate receptor 2
Gene Name
GRM2
Secondarily
Gene Name
Gprc1b
Mglur2
Sequence
MESLLGFLALLLLWGAVAEGPAKKVLTLEGDLVLGGLFPVHQKGGPAEECGPVNEHRGIQRLEAMLFALDRINRDPHLLPGVRLGAHILDSCSKDTHALEQALDFVRASLSRGADGSRHICPDGSYATHSDAPTAVTGVIGGSYSDVSIQVANLLRLFQIPQISYASTSAKLSDKSRYDYFARTVPPDFFQAKAMAEILRFFNWTYVSTVASEGDYGETGIEAFELEARARNICVATSEKVGRAMSRAAFEGVVRALLQKPSARVAVLFTRSEDARELLAATQRLNASFTWVASDGWGALESVVAGSERAAEGAITIELASYPISDFASYFQSLDPWNNSRNPWFREFWEERFHCSFRQRDCAAHSLRAVPFEQESKIMFVVNAVYAMAHALHNMHRALCPNTTHLCDAMRPVNGRRLYKDFVLNVKFDAPFRPADTDDEVRFDRFGDGIGRYNIFTYLRAGSGRYRYQKVGYWAEGLTLDTSFIPWASPSAGPLPASRCSEPCLQNEVKSVQPGEVCCWLCIPCQPYEYRLDEFTCADCGLGYWPNASLTGCFELPQEYIRWGDAWAVGPVTIACLGALATLFVLGVFVRHNATPVVKASGRELCYILLGGVFLCYCMTFVFIAKPSTAVCTLRRLGLGTAFSVCYSALLTKTNRIARIFGGAREGAQRPRFISPASQVAICLALISGQLLIVAAWLVVEAPGTGKETAPERREVVTLRCNHRDASMLGSLAYNVLLIALCTLYAFKTRKCPENFNEAKFIGFTMYTTCIIWLAFLPIFYVTSSDYRVQTTTMCVSVSLSGSVVLGCLFAPKLHIILFQPQKNVVSHRAPTSRFGSAAPRASANLGQGSGSQFVPTVCNGREVVDSTTSSL
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Organism
Rattus norvegicus, Rat
Protein Classification
Membrane receptor
>
Family C G protein-coupled receptor
>
Small molecule receptor (family C GPCR)
>
Neurotransmitter receptor (family C GPCR)
>
Metabotropic glutamate receptor
Function
G-protein coupled receptor for glutamate. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Signaling inhibits adenylate cyclase activity. May mediate suppression of neurotransmission or may be involved in synaptogenesis or synaptic stabilization.
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Uniprot ID
P31421
Ensembl ID
ENSG00000164082
Subcellular Location
Cell membrane
Synapse
Cell projection
Dendrite
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0076675
(1S,2S,5R,6S)-2-Amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H11NO4
 2
1
EC50 = 18.3 nM
   TI
   LI
   LO
   TS
2
Ki = 23.4 nM
   TI
   LI
   LO
   TS
CP0428983
(+/-)-2-Amino-6-fluoro-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H10FNO5
 2
1
EC50 = 21 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0399772
2-[1-Amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-cyclopropanecarboxylic acid
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C20H19NO5
 2
1
EC50 = 50.3 nM
   TI
   LI
   LO
   TS
2
Ki = 3.72 nM
   TI
   LI
   LO
   TS
CP0373675
(1S,2R,3R,5R,6S)-2-amino-3-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H10FNO4
 2
1
EC50 = 4490 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0492666
(1S,2S,3R,5R,6S)-2-amino-3-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H10FNO4
 2
1
EC50 = 17100 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0384897
(+/-)-2-Amino-3,3-difluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H9F2NO4
 2
1
EC50 = 36200 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0406282
(+/-)-2-Amino-6-methyl-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C9H13NO4
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0140442
(+)-2-Amino-3-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H10FNO4
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
Ki = 47.7 nM
   TI
   LI
   LO
   TS
CP0374563
(+)-2-Amino-6-fluoro-4-oxo-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H8FNO5
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
Ki = 3.3 nM
   TI
   LI
   LO
   TS
CP0409272
(+)-2-Amino-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H10FNO4
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
Ki = 22.5 nM
   TI
   LI
   LO
   TS
CP0211752
(1R,2R,3R,5R,6R)-2-Amino-3-(3,4-dichloro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C15H14Cl2FNO5
 3
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 = 20 nM
   TI
   LI
   LO
   TS
3
Ki = 2.38 nM
   TI
   LI
   LO
   TS
CP0377729
(1S,2S)-2-((S)-1-amino-1-carboxy-2-(9H-xanthen-9-yl)ethyl)cyclopropanecarboxylic acid
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C20H19NO5
 3
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 = 23.2 nM
   TI
   LI
   LO
   TS
3
Ki = 3.13 nM
   TI
   LI
   LO
   TS
CP0391913
(1R,2R,3R,5R,6R)-2-Amino-3-benzhydryloxy-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C21H20FNO5
 3
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 = 24.4 nM
   TI
   LI
   LO
   TS
3
Ki = 2.58 nM
   TI
   LI
   LO
   TS
CP0392388
(1R,2R,3R,5R,6R)-2-Amino-3-(3,4-difluoro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C15H14F3NO5
 3
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 = 40.8 nM
   TI
   LI
   LO
   TS
3
Ki = 2.27 nM
   TI
   LI
   LO
   TS
CP0406578
(1R,2R,3R,5R,6R)-2-Amino-3-(4-chloro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C15H15ClFNO5
 3
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 = 29.1 nM
   TI
   LI
   LO
   TS
3
Ki = 3.17 nM
   TI
   LI
   LO
   TS
CP0497432
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C8H10FNO5
 3
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 = 476 nM
   TI
   LI
   LO
   TS
3
Ki = 32.9 nM
   TI
   LI
   LO
   TS
CP0231490
7,8-dichloro-4-(3-(2-methylpyridin-4-yl)phenyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C21H15Cl2N3O
 1
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
CP0101907
7-methyl-4-(3-(pyridin-3-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C22H16F3N3O
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0202837
4-(3-(2,6-dimethylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C24H20F3N3O
 2
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
2
IC50 < 10 nM
   TI
   LI
   LO
   TS
CP0237661
8-chloro-4-(3-(pyridin-4-yl)phenyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C20H14ClN3O
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0053384
7-methyl-4-(3-(2-methylpyridin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C23H18F3N3O
 2
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
2
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0297209
4-(3-(2-ethyl-6-methylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C25H22F3N3O
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0336097
4-(3-(2-cyclopropyl-6-methylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C26H22F3N3O
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0218960
4-(3-(2-benzylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C29H22F3N3O
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0295951
4-(3-(2-ethylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C24H20F3N3O
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0336098
4-(3-(2-(methoxymethyl)-6-methylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C25H22F3N3O2
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0337808
7-methyl-4-(3-(6-methylpyridin-3-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C23H18F3N3O
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0530818
8-[2-(4-fluorophenyl)ethynyl]-4-[3-(triazol-1-yl)phenyl]-1,3-dihydro-1,5-benzodiazepin-2-one
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C25H16FN5O
 1
1
IC50 = 6 nM
   TI
   LI
   LO
   TS
CP0053390
4-(3-(2-cyclopropylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C25H20F3N3O
 1
1
IC50 = 6 nM
   TI
   LI
   LO
   TS
CP0295952
4-(3-(2-(methoxymethyl)pyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C24H20F3N3O2
 1
1
IC50 = 6 nM
   TI
   LI
   LO
   TS
CP0101910
4-(3-(2-cyclopentylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C27H24F3N3O
 1
1
IC50 = 7 nM
   TI
   LI
   LO
   TS
CP0237659
4-(3-(2,6-dimethylpyridin-4-yl)phenyl)-7,8-bis(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C24H17F6N3O
 1
1
IC50 = 7 nM
   TI
   LI
   LO
   TS
CP0232347
7-ethoxy-4-(3-(2-methylpyridin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C24H20F3N3O2
 1
1
IC50 = 8 nM
   TI
   LI
   LO
   TS
CP0338876
7-ethoxy-4-(3-(pyridin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C23H18F3N3O2
 2
1
IC50 = 8 nM
   TI
   LI
   LO
   TS
2
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0371812
8-[2-(4-fluorophenyl)ethynyl]-4-(3-imidazol-1-ylphenyl)-1,3-dihydro-1,5-benzodiazepin-2-one
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C26H17FN4O
 1
1
IC50 = 9 nM
   TI
   LI
   LO
   TS
CP0036327
7-methyl-4-(3-(3-methylisoxazol-5-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C21H16F3N3O2
 1
1
IC50 = 9 nM
   TI
   LI
   LO
   TS
CP0052924
4-(3-(6-methoxypyridin-3-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C23H18F3N3O2
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0053392
4-(3-(6-isopropylpyridin-3-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C25H22F3N3O
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0101909
4-(3-(2-isopropylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C25H22F3N3O
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0059417
8-(2-fluorophenyl)-4-(3-imidazol-1-ylphenyl)-1,3-dihydro-1,5-benzodiazepin-2-one
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C24H17FN4O
 1
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
CP0101908
7-methyl-4-(3-(pyridin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C22H16F3N3O
 1
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
CP0101912
4-(3-(1H-imidazol-1-yl)phenyl)-8-((4-fluorophenyl)ethynyl)-7-hydroxy-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C26H17FN4O2
 3
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
2
IC50 = 24 nM
   TI
   LI
   LO
   TS
3
IC50 = 26 nM
   TI
   LI
   LO
   TS
CP0162027
4-(3-(1H-1,2,3-triazol-1-yl)phenyl)-8-(2-fluorophenyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C23H16FN5O
 4
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
2
IC50 = 16 nM
   TI
   LI
   LO
   TS
3
IC50 = 22 nM
   TI
   LI
   LO
   TS
4
IC50 = 27 nM
   TI
   LI
   LO
   TS
CP0472153
4-(3-imidazol-1-ylphenyl)-8-(2-phenylethynyl)-1,3-dihydro-1,5-benzodiazepin-2-one
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C26H18N4O
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0335052
4-(3-(2-(2-hydroxypropan-2-yl)pyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C25H22F3N3O2
 1
1
IC50 = 14 nM
   TI
   LI
   LO
   TS
CP0295953
4-(3-(2-(hydroxymethyl)-6-methylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C24H20F3N3O2
 1
1
IC50 = 15 nM
   TI
   LI
   LO
   TS
CP0038458
4-(3-(2-methoxypyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C23H18F3N3O2
 1
1
IC50 = 16 nM
   TI
   LI
   LO
   TS
CP0283397
7-methyl-4-(3-(pyrazin-2-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C21H15F3N4O
 1
1
IC50 = 16 nM
   TI
   LI
   LO
   TS
CP0079531
(E)-3-(4-oxo-7-(2-phenylethynyl)-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C24H15N3O
 2
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
2
IC50 = 34 nM
   TI
   LI
   LO
   TS
CP0510824
(E)-3-(8-(cyanomethoxy)-4-oxo-7-(2-phenylethynyl)-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C26H16N4O2
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0371810
2-[[4-(3-imidazol-1-ylphenyl)-2-oxo-8-(2-phenylethynyl)-1,3-dihydro-1,5-benzodiazepin-7-yl]oxy]acetonitrile
   Show/Hide
C28H19N5O2
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0161929
4-(3-(6-ethylpyridin-3-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C24H20F3N3O
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0297211
4-(3-(2-(hydroxymethyl)pyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C23H18F3N3O2
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0368814
4-(3-(7-methyl-2-oxo-8-(trifluoromethyl)-2,3-dihydro-1H-benzo[b][1,4]diazepin-4-yl)phenyl)picolinonitrile
   Show/Hide
C23H15F3N4O
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0059416
4-(3-(1H-imidazol-1-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C20H15F3N4O
 1
1
IC50 = 19 nM
   TI
   LI
   LO
   TS
CP0311023
8-[2-(4-fluorophenyl)ethynyl]-7-hydroxy-4-[3-(triazol-1-yl)phenyl]-1,3-dihydro-1,5-benzodiazepin-2-one
   Show/Hide
C25H16FN5O2
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0472152
8-[2-(2-fluorophenyl)ethynyl]-4-(3-imidazol-1-ylphenyl)-1,3-dihydro-1,5-benzodiazepin-2-one
   Show/Hide
C26H17FN4O
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0039555
4-(3-(6-cyclopropylpyridin-3-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C25H20F3N3O
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0499045
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-(naphthalen-2-ylmethoxy)-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C19H18FNO5
 2
1
IC50 = 22.7 nM
   TI
   LI
   LO
   TS
2
Ki = 2.53 nM
   TI
   LI
   LO
   TS
CP0438863
4-(3-imidazol-1-ylphenyl)-7-(2-methoxyethoxy)-8-(2-phenylethynyl)-1,3-dihydro-1,5-benzodiazepin-2-one
   Show/Hide
C29H24N4O3
 1
1
IC50 = 23 nM
   TI
   LI
   LO
   TS
CP0373237
(E)-N-tert-butyl-2-(4-(3-cyanophenyl)-2-oxo-8-(2-phenylethynyl)-2,3-dihydro-1H-benzo[b][1,4]diazepin-7-yloxy)acetamide
   Show/Hide
C30H26N4O3
 1
1
IC50 = 26 nM
   TI
   LI
   LO
   TS
CP0373238
(E)-4-phenyl-8-(2-phenylethynyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C23H16N2O
 1
1
IC50 = 26 nM
   TI
   LI
   LO
   TS
CP0237670
4-(3-(pyridin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C21H14F3N3O
 2
1
IC50 = 26 nM
   TI
   LI
   LO
   TS
2
IC50 = 101 nM
   TI
   LI
   LO
   TS
CP0510825
(E)-3-(8-(2-methoxyethoxy)-4-oxo-7-(2-phenylethynyl)-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C27H21N3O3
 1
1
IC50 = 28 nM
   TI
   LI
   LO
   TS
CP0511442
(E)-3-(7-(2-(2-fluorophenyl)ethynyl)-4-oxo-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C24H14FN3O
 1
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
CP0295955
4-(3-(2,2'-bipyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C22H16F3N3O
 1
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
CP0467707
(E)-3-(4-oxo-7-(2-(thiophen-2-yl)ethynyl)-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C22H13N3OS
 1
1
IC50 = 32 nM
   TI
   LI
   LO
   TS
CP0510826
(E)-3-(7-(2-(4-fluorophenyl)ethynyl)-4-oxo-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C24H14FN3O
 1
1
IC50 = 34 nM
   TI
   LI
   LO
   TS
CP0205609
8-(2-fluorophenyl)-7-hydroxy-4-(3-imidazol-1-ylphenyl)-1,3-dihydro-1,5-benzodiazepin-2-one
   Show/Hide
C24H17FN4O2
 1
1
IC50 = 35 nM
   TI
   LI
   LO
   TS
CP0511612
7-(dimethylamino)-8-(2-phenylethynyl)-4-[3-(triazol-1-yl)phenyl]-1,3-dihydro-1,5-benzodiazepin-2-one
   Show/Hide
C27H22N6O
 1
1
IC50 = 36 nM
   TI
   LI
   LO
   TS
CP0295954
4-(3-(2-methylpyridin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C22H16F3N3O
 1
1
IC50 = 36 nM
   TI
   LI
   LO
   TS
CP0349551
4-(3-(1H-1,2,3-triazol-1-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C19H14F3N5O
 1
1
IC50 = 39 nM
   TI
   LI
   LO
   TS
CP0392972
(E)-3-(4-oxo-7-(2-phenylethynyl)-8-thiomorpholino-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C28H22N4OS
 1
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
CP0472150
8-[2-(4-fluorophenyl)ethynyl]-7-(2-hydroxyethoxy)-4-(3-imidazol-1-ylphenyl)-1,3-dihydro-1,5-benzodiazepin-2-one
   Show/Hide
C28H21FN4O3
 1
1
IC50 = 46 nM
   TI
   LI
   LO
   TS
CP0336099
7-methyl-4-(3-(6-(pyrimidin-5-yl)pyridin-3-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C21H15F3N4O
 1
1
IC50 = 48 nM
   TI
   LI
   LO
   TS
CP0332809
7-methyl-4-(3-(pyrimidin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C21H15F3N4O
 1
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
CP0521578
(E)-3-(8-(dimethylamino)-4-oxo-7-(2-phenylethynyl)-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C26H20N4O
 1
1
IC50 = 60 nM
   TI
   LI
   LO
   TS
CP0541780
(E)-3-(4-oxo-7-(2-p-tolylethynyl)-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C25H17N3O
 1
1
IC50 = 64 nM
   TI
   LI
   LO
   TS
CP0536199
7-(2-hydroxyethoxy)-4-(3-imidazol-1-ylphenyl)-8-(2-phenylethynyl)-1,3-dihydro-1,5-benzodiazepin-2-one
   Show/Hide
C28H22N4O3
 1
1
IC50 = 64 nM
   TI
   LI
   LO
   TS
CP0510827
(E)-3-(7-(2-(4-methoxyphenyl)ethynyl)-4-oxo-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C25H17N3O2
 1
1
IC50 = 68 nM
   TI
   LI
   LO
   TS
CP0516505
8-[2-(4-fluorophenyl)ethynyl]-4-[3-(tetrazol-1-yl)phenyl]-1,3-dihydro-1,5-benzodiazepin-2-one
   Show/Hide
C24H15FN6O
 1
1
IC50 = 72 nM
   TI
   LI
   LO
   TS
CP0237672
7-methyl-4-(3-(pyridazin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C21H15F3N4O
 1
1
IC50 = 72 nM
   TI
   LI
   LO
   TS
CP0161928
4-(3-(1H-1,2,4-triazol-1-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C19H14F3N5O
 1
1
IC50 = 75 nM
   TI
   LI
   LO
   TS
CP0521579
(E)-3-(7-(2-(2-chlorophenyl)ethynyl)-4-oxo-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C24H14ClN3O
 1
1
IC50 = 76 nM
   TI
   LI
   LO
   TS
CP0522335
(E)-4-(3-chlorophenyl)-8-(2-phenylethynyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C23H15ClN2O
 1
1
IC50 = 80 nM
   TI
   LI
   LO
   TS
CP0501786
(E)-3-(8-(4-methoxypiperidin-1-yl)-4-oxo-7-(2-phenylethynyl)-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C30H26N4O2
 1
1
IC50 = 82 nM
   TI
   LI
   LO
   TS
CP0501785
(E)-3-(8-methoxy-4-oxo-7-(2-phenylethynyl)-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C25H17N3O2
 1
1
IC50 = 92 nM
   TI
   LI
   LO
   TS
CP0371811
8-[2-(4-fluorophenyl)ethynyl]-4-[3-(1,2,4-triazol-1-yl)phenyl]-1,3-dihydro-1,5-benzodiazepin-2-one
   Show/Hide
C25H16FN5O
 1
1
IC50 = 98 nM
   TI
   LI
   LO
   TS
CP0472151
8-[2-(4-fluorophenyl)ethynyl]-4-[3-(4-methylimidazol-1-yl)phenyl]-1,3-dihydro-1,5-benzodiazepin-2-one
   Show/Hide
C27H19FN4O
 1
1
IC50 = 98 nM
   TI
   LI
   LO
   TS
CP0293651
1-[(Z)-2-Cycloheptyloxy-2-(2,6-dichloro-phenyl)-vinyl]-1H-[1,2,4]triazole
   Show/Hide
C17H19Cl2N3O
 2
1
IC50 = 110 nM
   TI
   LI
   LO
   TS
2
IC50 = 500 nM
   TI
   LI
   LO
   TS
CP0491988
(1R,2R,3R,5R,6R)-2-Amino-3-benzyloxy-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H16FNO5
 2
1
IC50 = 131 nM
   TI
   LI
   LO
   TS
2
Ki = 7.14 nM
   TI
   LI
   LO
   TS
CP0438862
8-[2-(4-fluorophenyl)ethynyl]-7-[2-hydroxyethyl(methyl)amino]-4-(3-imidazol-1-ylphenyl)-1,3-dihydro-1,5-benzodiazepin-2-one
   Show/Hide
C29H24FN5O2
 1
1
IC50 = 140 nM
   TI
   LI
   LO
   TS
CP0505614
(E)-4-(3-iodophenyl)-8-(2-phenylethynyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C23H15IN2O
 1
1
IC50 = 154 nM
   TI
   LI
   LO
   TS
CP0501787
3-[8-(1,1-dioxo-1lambda6-thiomorpholin-4-yl)-4-oxo-7-phenylethynyl-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl]-benzonitrile
   Show/Hide
C28H22N4O3S
 1
1
IC50 = 160 nM
   TI
   LI
   LO
   TS
CP0237671
4-(3-(6-aminopyridin-3-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C22H17F3N4O
 1
1
IC50 = 160 nM
   TI
   LI
   LO
   TS
CP0394010
4-[3-(2,4-dimethylimidazol-1-yl)phenyl]-8-(2-phenylethynyl)-1,3-dihydro-1,5-benzodiazepin-2-one
   Show/Hide
C28H22N4O
 1
1
IC50 = 170 nM
   TI
   LI
   LO
   TS
CP0243343
4-(3-(1-methyl-1H-pyrazol-5-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C20H15F3N4O
 1
1
IC50 = 190 nM
   TI
   LI
   LO
   TS
CP0491986
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-methoxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C9H12FNO5
 2
1
IC50 = 229 nM
   TI
   LI
   LO
   TS
2
Ki = 39.2 nM
   TI
   LI
   LO
   TS
CP0438892
8-(2-phenylethynyl)-4-(3-(trifluoromethyl)phenyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C24H15F3N2O
 1
1
IC50 = 268 nM
   TI
   LI
   LO
   TS
CP0467706
(E)-3-(8-(4-methylpiperazin-1-yl)-4-oxo-7-(2-phenylethynyl)-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C29H25N5O
 1
1
IC50 = 278 nM
   TI
   LI
   LO
   TS
CP0484073
8-(4-fluorophenyl)-4-(3-imidazol-1-ylphenyl)-1,3-dihydro-1,5-benzodiazepin-2-one
   Show/Hide
C24H17FN4O
 1
1
IC50 = 299 nM
   TI
   LI
   LO
   TS
CP0438890
(E)-3-(4-oxo-7-(2-(thiazol-2-yl)ethynyl)-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C21H12N4OS
 1
1
IC50 = 300 nM
   TI
   LI
   LO
   TS
CP0405277
(E)-3-(4-oxo-7-(2-phenylethynyl)-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzamide
   Show/Hide
C24H17N3O2
 1
1
IC50 = 358 nM
   TI
   LI
   LO
   TS
CP0500554
(E)-4-(3-(morpholine-4-carbonyl)phenyl)-8-(2-phenylethynyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C28H23N3O3
 1
1
IC50 = 360 nM
   TI
   LI
   LO
   TS
CP0522333
(E)-3-(8-morpholino-4-oxo-7-(2-phenylethynyl)-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C28H22N4O2
 1
1
IC50 = 378 nM
   TI
   LI
   LO
   TS
CP0530817
8-[2-(4-fluorophenyl)ethynyl]-7-hydroxy-4-[3-[5-(hydroxymethyl)triazol-1-yl]phenyl]-1,3-dihydro-1,5-benzodiazepin-2-one
   Show/Hide
C26H18FN5O3
 1
1
IC50 = 378 nM
   TI
   LI
   LO
   TS
CP0511441
(E)-3-(7-(3-methylbut-3-en-1-ynyl)-4-oxo-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C21H15N3O
 1
1
IC50 = 400 nM
   TI
   LI
   LO
   TS
CP0438888
3-[4-oxo-8-(1-oxo-1lambda4-thiomorpholin-4-yl)-7-phenylethynyl-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl]-benzonitrile
   Show/Hide
C28H22N4O2S
 1
1
IC50 = 446 nM
   TI
   LI
   LO
   TS
CP0432271
1-[(Z)-2-Cycloheptyloxy-2-(2,4-dichloro-phenyl)-vinyl]-1H-[1,2,4]triazole
   Show/Hide
C17H19Cl2N3O
 1
1
IC50 = 470 nM
   TI
   LI
   LO
   TS
CP0392973
(E)-3-(7-(2-(2,4-difluorophenyl)ethynyl)-4-oxo-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C24H13F2N3O
 1
1
IC50 = 480 nM
   TI
   LI
   LO
   TS
CP0395350
1-[(Z)-2-Cyclohexyloxy-2-(2,6-dichloro-phenyl)-vinyl]-1H-[1,2,4]triazole
   Show/Hide
C16H17Cl2N3O
 1
1
IC50 = 580 nM
   TI
   LI
   LO
   TS
CP0496578
(E)-2-(4-(3-cyanophenyl)-2-oxo-8-(2-phenylethynyl)-2,3-dihydro-1H-benzo[b][1,4]diazepin-7-yloxy)acetic acid
   Show/Hide
C26H17N3O4
 1
1
IC50 = 600 nM
   TI
   LI
   LO
   TS
CP0394009
4-[3-(1-methylimidazol-2-yl)phenyl]-8-(2-phenylethynyl)-1,3-dihydro-1,5-benzodiazepin-2-one
   Show/Hide
C27H20N4O
 1
1
IC50 = 730 nM
   TI
   LI
   LO
   TS
CP0505613
(E)-3-(4-oxo-7-(2-(pyridin-2-yl)ethynyl)-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C23H14N4O
 1
1
IC50 = 870 nM
   TI
   LI
   LO
   TS
CP0522336
(E)-4-(3-methoxyphenyl)-8-(2-phenylethynyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C24H18N2O2
 1
1
IC50 = 962 nM
   TI
   LI
   LO
   TS
CP0525023
(E)-4-(3-(1-methylpiperazine-4-carbonyl)phenyl)-8-(2-phenylethynyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C29H26N4O2
 1
1
IC50 = 1040 nM
   TI
   LI
   LO
   TS
CP0524539
1-[(Z)-2-Cyclohexyloxy-2-(2,4-dichloro-phenyl)-vinyl]-1H-[1,2,4]triazole
   Show/Hide
C16H17Cl2N3O
 1
1
IC50 = 1050 nM
   TI
   LI
   LO
   TS
CP0428732
1-[(Z)-2-Cyclooctyloxy-2-(2,4-dichloro-phenyl)-vinyl]-1H-[1,2,4]triazole
   Show/Hide
C18H21Cl2N3O
 1
1
IC50 = 1210 nM
   TI
   LI
   LO
   TS
CP0414866
1-[(Z)-2-Cycloheptyloxy-2-(4-trifluoromethyl-phenyl)-vinyl]-1H-[1,2,4]triazole
   Show/Hide
C18H20F3N3O
 1
1
IC50 = 1380 nM
   TI
   LI
   LO
   TS
CP0510828
(E)-8-methyl-4-(3-(trifluoromethyl)phenyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C17H13F3N2O
 1
1
IC50 = 1530 nM
   TI
   LI
   LO
   TS
CP0448963
1-[(Z)-2-Benzyloxy-2-(2,6-dichloro-phenyl)-vinyl]-1H-[1,2,4]triazole
   Show/Hide
C17H13Cl2N3O
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0501784
(E)-2-(4-(3-cyanophenyl)-2-oxo-8-(2-phenylethynyl)-2,3-dihydro-1H-benzo[b][1,4]diazepin-7-yloxy)acetamide
   Show/Hide
C26H18N4O3
 1
1
IC50 = 2400 nM
   TI
   LI
   LO
   TS
CP0509448
1-[(Z)-2-Cyclopentyloxy-2-(2,4-dichloro-phenyl)-vinyl]-1H-[1,2,4]triazole
   Show/Hide
C15H15Cl2N3O
 1
1
IC50 = 2550 nM
   TI
   LI
   LO
   TS
CP0504842
1-[(Z)-2-Benzyloxy-2-(2,4-dichloro-phenyl)-vinyl]-1H-tetrazole
   Show/Hide
C16H12Cl2N4O
 1
1
IC50 = 2680 nM
   TI
   LI
   LO
   TS
CP0438891
(E)-4-(3-chlorophenyl)-8-methyl-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C16H13ClN2O
 1
1
IC50 = 2820 nM
   TI
   LI
   LO
   TS
CP0501808
(E)-3-(7-methyl-4-oxo-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C17H13N3O
 1
1
IC50 = 2900 nM
   TI
   LI
   LO
   TS
CP0375990
2-[(Z)-2-Butoxy-2-(4-chloro-phenyl)-vinyl]-2H-tetrazole
   Show/Hide
C13H15ClN4O
 1
1
IC50 = 3160 nM
   TI
   LI
   LO
   TS
CP0496893
1-[(Z)-2-(2,4-Dichloro-phenyl)-2-isopropoxy-vinyl]-1H-[1,2,4]triazole
   Show/Hide
C13H13Cl2N3O
 2
1
IC50 = 6000 nM
   TI
   LI
   LO
   TS
2
IC50 = 11500 nM
   TI
   LI
   LO
   TS
CP0295902
8-methyl-4-phenyl-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C16H14N2O
 1
1
IC50 = 6400 nM
   TI
   LI
   LO
   TS
CP0500553
(E)-4-(3-methoxyphenyl)-8-methyl-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C17H16N2O2
 1
1
IC50 = 6580 nM
   TI
   LI
   LO
   TS
CP0522334
(E)-3-(7-(3-hydroxy-3-methylbut-1-ynyl)-4-oxo-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
   Show/Hide
C21H17N3O2
 1
1
IC50 = 26000 nM
   TI
   LI
   LO
   TS
CP0406519
1-[2-(2,6-dichloro-phenyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidin-6-yl]-ethanone
   Show/Hide
C25H25Cl2N3O3S
 2
1
IC50 = 30000 nM
   TI
   LI
   LO
   TS
2
Ki = 7000 nM
   TI
   LI
   LO
   TS
CP0501079
1-[(Z)-2-(2,4-Difluoro-phenyl)-2-isopropoxy-vinyl]-1H-[1,2,4]triazole
   Show/Hide
C13H13F2N3O
 1
1
IC50 = 75000 nM
   TI
   LI
   LO
   TS
CP0504186
1-[(Z)-2-(2,4-Dimethoxy-phenyl)-2-isopropoxy-vinyl]-1H-[1,2,4]triazole
   Show/Hide
C15H19N3O3
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0469288
(1R,2R,3R,5R,6R)-2-Amino-3-(3-carboxy-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C16H16FNO7
 1
1
Ki = 1.06 nM
   TI
   LI
   LO
   TS
CP0429935
(1R,2R,3R,5R,6R)-2-Amino-3-[(R)-1-(3,4-dichloro-phenyl)-ethoxy]-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C16H16Cl2FNO5
 1
1
Ki = 1.45 nM
   TI
   LI
   LO
   TS
CP0392054
(1R,2R,3R,5R,6R)-2-Amino-3-[(R)-1-(3,4-dichloro-phenyl)-butoxy]-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C18H20Cl2FNO5
 1
1
Ki = 1.48 nM
   TI
   LI
   LO
   TS
CP0502825
(1R,2R,3R,5R,6R)-2-Amino-3-[(R)-1-(3,4-dichloro-phenyl)-propoxy]-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C17H18Cl2FNO5
 1
1
Ki = 1.61 nM
   TI
   LI
   LO
   TS
CP0436519
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-((S)-1-naphthalen-2-yl-ethoxy)-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C20H20FNO5
 1
1
Ki = 1.79 nM
   TI
   LI
   LO
   TS
CP0500540
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-((R)-1-naphthalen-2-yl-ethoxy)-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C20H20FNO5
 1
1
Ki = 2.01 nM
   TI
   LI
   LO
   TS
CP0405838
(1R,2R,3R,5R,6R)-2-Amino-3-[bis-(3,4-dichloro-phenyl)-methoxy]-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C21H16Cl4FNO5
 1
1
Ki = 2.61 nM
   TI
   LI
   LO
   TS
CP0406579
(1R,2R,3R,5R,6R)-2-Amino-3-(3-cyano-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C16H15FN2O5
 1
1
Ki = 2.94 nM
   TI
   LI
   LO
   TS
CP0497422
(1R,2R,3R,5R,6R)-2-Amino-3-[(S)-1-(3,4-dichloro-phenyl)-butoxy]-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C18H20Cl2FNO5
 1
1
Ki = 3.05 nM
   TI
   LI
   LO
   TS
CP0492972
(1R,2R,3R,5R,6R)-2-Amino-3-[(S)-1-(3,4-dichloro-phenyl)-propoxy]-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C17H18Cl2FNO5
 1
1
Ki = 3.12 nM
   TI
   LI
   LO
   TS
CP0491991
(1R,2R,3R,5R,6R)-2-Amino-3-(3-chloro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H15ClFNO5
 1
1
Ki = 3.28 nM
   TI
   LI
   LO
   TS
CP0506238
(1R,2R,3R,5R,6R)-2-Amino-3-(3-chloro-4-fluoro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H14ClF2NO5
 1
1
Ki = 3.57 nM
   TI
   LI
   LO
   TS
CP0496872
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-(3,4,5-trichloro-benzyloxy)-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H13Cl3FNO5
 1
1
Ki = 3.67 nM
   TI
   LI
   LO
   TS
CP0497433
(1R,2R,3R,5R,6R)-2-Amino-3-[bis-(4-chloro-phenyl)-methoxy]-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C21H18Cl2FNO5
 1
1
Ki = 3.75 nM
   TI
   LI
   LO
   TS
CP0440314
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-pentafluorophenylmethoxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H11F6NO5
 1
1
Ki = 3.77 nM
   TI
   LI
   LO
   TS
CP0497434
(1R,2R,3R,5R,6R)-2-Amino-3-[bis-(4-fluoro-phenyl)-methoxy]-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C21H18F3NO5
 1
1
Ki = 3.79 nM
   TI
   LI
   LO
   TS
CP0500805
(1R,2R,3R,5R,6R)-2-Amino-3-(2,4-dichloro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H14Cl2FNO5
 1
1
Ki = 3.89 nM
   TI
   LI
   LO
   TS
CP0550894
(1R,2R,3R,5R,6R)-2-Amino-3-(4-chloro-3-fluoro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H14ClF2NO5
 1
1
Ki = 4.02 nM
   TI
   LI
   LO
   TS
CP0491993
(1R,2R,3R,5R,6R)-2-Amino-3-(biphenyl-2-ylmethoxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C21H20FNO5
 1
1
Ki = 4.07 nM
   TI
   LI
   LO
   TS
CP0374731
(1R,2R,3R,5R,6R)-2-Amino-3-(2,3-difluoro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H14F3NO5
 1
1
Ki = 4.25 nM
   TI
   LI
   LO
   TS
CP0485762
(1R,2R,3R,5R,6R)-2-Amino-3-(2,6-dichloro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H14Cl2FNO5
 1
1
Ki = 4.3 nM
   TI
   LI
   LO
   TS
CP0497294
(1R,2R,3R,5R,6R)-2-Amino-3-(2,3-dichloro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H14Cl2FNO5
 1
1
Ki = 4.35 nM
   TI
   LI
   LO
   TS
CP0541498
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-(3-methyl-benzyloxy)-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C16H18FNO5
 1
1
Ki = 4.53 nM
   TI
   LI
   LO
   TS
CP0445907
(1R,2R,3R,5R,6R)-2-Amino-3-(2,4-difluoro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H14F3NO5
 1
1
Ki = 4.71 nM
   TI
   LI
   LO
   TS
CP0485010
(1R,2R,3R,5R,6R)-2-Amino-3-(3-bromo-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H15BrFNO5
 1
1
Ki = 4.71 nM
   TI
   LI
   LO
   TS
CP0541488
(1R,2R,3R,5R,6R)-2-Amino-3-(2-chloro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H15ClFNO5
 1
1
Ki = 4.99 nM
   TI
   LI
   LO
   TS
CP0394652
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-propoxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C11H16FNO5
 1
1
Ki = 5.17 nM
   TI
   LI
   LO
   TS
CP0379235
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-(naphthalen-1-ylmethoxy)-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C19H18FNO5
 1
1
Ki = 5.36 nM
   TI
   LI
   LO
   TS
CP0491990
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-(4-fluoro-benzyloxy)-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H15F2NO5
 1
1
Ki = 5.55 nM
   TI
   LI
   LO
   TS
CP0521126
(1R,2R,3R,5R,6R)-2-Amino-3-(3,5-dichloro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H14Cl2FNO5
 1
1
Ki = 5.61 nM
   TI
   LI
   LO
   TS
CP0511387
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-(3-trifluoromethyl-benzyloxy)-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C16H15F4NO5
 1
1
Ki = 5.72 nM
   TI
   LI
   LO
   TS
CP0491946
(1R,2R,3R,5R,6R)-2-Amino-3-[(S)-1-(3,4-dichloro-phenyl)-ethoxy]-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C16H16Cl2FNO5
 1
1
Ki = 5.81 nM
   TI
   LI
   LO
   TS
CP0469289
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-(3-methoxy-benzyloxy)-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C16H18FNO6
 1
1
Ki = 5.92 nM
   TI
   LI
   LO
   TS
CP0435564
(1R,2R,3R,5R,6R)-2-Amino-3-sec-butoxy-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C12H18FNO5
 1
1
Ki = 6.68 nM
   TI
   LI
   LO
   TS
CP0403586
(1R,2R,3R,5R,6R)-2-Amino-3-(2,6-difluoro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H14F3NO5
 1
1
Ki = 7.02 nM
   TI
   LI
   LO
   TS
CP0491987
(1R,2R,3R,5R,6R)-3-Allyloxy-2-amino-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C11H14FNO5
 1
1
Ki = 7.07 nM
   TI
   LI
   LO
   TS
CP0374514
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-(3-phenoxy-benzyloxy)-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C21H20FNO6
 1
1
Ki = 7.15 nM
   TI
   LI
   LO
   TS
CP0494599
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-(3-nitro-benzyloxy)-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H15FN2O7
 1
1
Ki = 7.87 nM
   TI
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   LO
   TS
CP0543248
(1R,2R,3R,5R,6R)-2-Amino-3-cyclopentyloxy-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C13H18FNO5
 1
1
Ki = 8.57 nM
   TI
   LI
   LO
   TS
CP0502898
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-(thiophen-2-ylmethoxy)-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C13H14FNO5S
 1
1
Ki = 8.79 nM
   TI
   LI
   LO
   TS
CP0440234
(1R,2R,3R,5R,6R)-2-Amino-3-(biphenyl-3-ylmethoxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C21H20FNO5
 1
1
Ki = 9.34 nM
   TI
   LI
   LO
   TS
CP0497452
(1R,2R,3R,5R,6R)-2-Amino-6-fluoro-3-(3-phenyl-propoxy)-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C17H20FNO5
 1
1
Ki = 9.83 nM
   TI
   LI
   LO
   TS
CP0437051
(1R,2R,3R,5R,6R)-2-Amino-3-(2,5-dichloro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H14Cl2FNO5
 1
1
Ki = 11.8 nM
   TI
   LI
   LO
   TS
CP0509748
(1R,2R,3R,5R,6R)-2-Amino-3-(3,5-difluoro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H14F3NO5
 1
1
Ki = 12.4 nM
   TI
   LI
   LO
   TS
CP0445908
(1R,2R,3R,5R,6R)-2-Amino-3-(2,5-difluoro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H14F3NO5
 1
1
Ki = 14.4 nM
   TI
   LI
   LO
   TS
CP0499951
(1R,2R,3R,5R,6R)-2-Amino-3-(3-amino-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H17FN2O5
 1
1
Ki = 15.4 nM
   TI
   LI
   LO
   TS
CP0432785
(1R,2R,3S,5R,6R)-2-Amino-3-(3,4-dichloro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C15H14Cl2FNO5
 1
1
Ki = 17.1 nM
   TI
   LI
   LO
   TS
CP0497251
(1R,2R,3S,5R,6R)-2-Amino-3-[bis-(4-chloro-phenyl)-methoxy]-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C21H18Cl2FNO5
 1
1
Ki = 20.2 nM
   TI
   LI
   LO
   TS
CP0485011
(1R,2R,3R,5R,6R)-2-Amino-3-(biphenyl-4-ylmethoxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C21H20FNO5
 1
1
Ki = 25.6 nM
   TI
   LI
   LO
   TS
CP0433546
(1R,2S,4R,5R)-2-Amino-6-(R)-fluoro-3-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C8H10FNO5
 1
1
Ki = 105 nM
   TI
   LI
   LO
   TS
CP0497250
(1R,2R,3S,5R,6R)-2-Amino-6-fluoro-3-methoxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
   Show/Hide
C9H12FNO5
 1
1
Ki = 190 nM
   TI
   LI
   LO
   TS
CP0448141
2-(2,4-Dichloro-phenyl)-5-(2-methoxy-phenyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid 2-dimethylamino-ethyl ester
   Show/Hide
C25H25Cl2N3O3S
 1
1
Ki = 1000 nM
   TI
   LI
   LO
   TS
CP0535343
2-(2,6-Dichloro-phenyl)-7-ethyl-5-(2-methoxy-phenyl)-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid 2-dimethylamino-ethyl ester
   Show/Hide
C26H27Cl2N3O3S
 1
1
Ki = 1000 nM
   TI
   LI
   LO
   TS
CP0516104
2-(2,6-Dichloro-phenyl)-5-(2-methoxy-phenyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid 2-dimethylamino-ethyl ester
   Show/Hide
C25H25Cl2N3O3S
 1
1
Ki = 1500 nM
   TI
   LI
   LO
   TS
CP0462808
2-(2,6-Dichloro-phenyl)-5-(3-methoxy-phenyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid 2-dimethylamino-ethyl ester
   Show/Hide
C25H25Cl2N3O3S
 1
1
Ki = 2000 nM
   TI
   LI
   LO
   TS
CP0466563
2-(2,6-Dichloro-phenyl)-5-(2-isopropoxy-phenyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid 2-dimethylamino-ethyl ester
   Show/Hide
C27H29Cl2N3O3S
 1
1
Ki = 2000 nM
   TI
   LI
   LO
   TS
CP0535617
5-(2-Chloro-phenyl)-2-(2,6-dichloro-phenyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid 2-dimethylamino-ethyl ester
   Show/Hide
C24H22Cl3N3O2S
 1
1
Ki = 2000 nM
   TI
   LI
   LO
   TS
CP0380437
2-(2,6-Dichloro-phenyl)-5-(2-methoxy-phenyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid 3-dimethylamino-propyl ester
   Show/Hide
C26H27Cl2N3O3S
 1
1
Ki = 2400 nM
   TI
   LI
   LO
   TS
CP0526091
2-(2,6-Dichloro-phenyl)-5-(2-ethoxy-phenyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid 2-dimethylamino-ethyl ester
   Show/Hide
C26H27Cl2N3O3S
 1
1
Ki = 3000 nM
   TI
   LI
   LO
   TS
CP0559676
2-(2,6-Dichloro-phenyl)-5-(2-fluoro-phenyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid 2-dimethylamino-ethyl ester
   Show/Hide
C24H22Cl2FN3O2S
 1
1
Ki = 3200 nM
   TI
   LI
   LO
   TS
CP0451223
2-(2,6-Dichloro-phenyl)-7-isopropyl-5-(2-methoxy-phenyl)-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid 2-dimethylamino-ethyl ester
   Show/Hide
C27H29Cl2N3O3S
 1
1
Ki = 4000 nM
   TI
   LI
   LO
   TS
CP0460067
2-(4-Chloro-phenyl)-5-(2-methoxy-phenyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid 2-dimethylamino-ethyl ester
   Show/Hide
C25H26ClN3O3S
 1
1
Ki = 4000 nM
   TI
   LI
   LO
   TS
CP0498119
2-(2,6-Dichloro-phenyl)-5-(2-methoxy-phenyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid ethyl ester
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C23H20Cl2N2O3S
 1
1
Ki = 4000 nM
   TI
   LI
   LO
   TS
CP0408490
2-(2,6-Dichloro-phenyl)-7-methyl-5-o-tolyl-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid 2-dimethylamino-ethyl ester
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C25H25Cl2N3O2S
 1
1
Ki = 8000 nM
   TI
   LI
   LO
   TS
CP0480629
7-Benzoyl-2-(2,6-dichloro-phenyl)-5-(2-methoxy-phenyl)-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid 2-dimethylamino-ethyl ester
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C31H27Cl2N3O4S
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0515290
2-(2,6-Dichloro-phenyl)-5-(2-methoxy-phenyl)-7-methyl-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid (2-dimethylamino-ethyl)-amide
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C25H26Cl2N4O2S
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0485761
(1S,2S,3S,5S,6S)-2-Amino-3-(3,4-dichloro-benzyloxy)-6-fluoro-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
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C15H14Cl2FNO5
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0091883
(1R,2R)-3-((S)-Amino-carboxy-methyl)-cyclopropane-1,2-dicarboxylic acid
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C7H9NO6
 1
1 EC50 = 350 nM
CP0002355
(2S)-2-aminopentanedioic acid
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C5H9NO4
 2
1 EC50 = 4000 nM
2 EC50 = 16090 nM
CP0101907
7-methyl-4-(3-(pyridin-3-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C22H16F3N3O
 1
1 IC50 = 2 nM
CP0202837
4-(3-(2,6-dimethylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C24H20F3N3O
 1
1 IC50 = 2 nM
CP0297209
4-(3-(2-ethyl-6-methylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C25H22F3N3O
 1
1 IC50 = 2 nM
CP0336097
4-(3-(2-cyclopropyl-6-methylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C26H22F3N3O
 1
1 IC50 = 2 nM
CP0053384
7-methyl-4-(3-(2-methylpyridin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C23H18F3N3O
 1
1 IC50 = 4 nM
CP0101908
7-methyl-4-(3-(pyridin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C22H16F3N3O
 1
1 IC50 = 4 nM
CP0101909
4-(3-(2-isopropylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C25H22F3N3O
 1
1 IC50 = 4 nM
CP0231490
7,8-dichloro-4-(3-(2-methylpyridin-4-yl)phenyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C21H15Cl2N3O
 1
1 IC50 = 4 nM
CP0338876
7-ethoxy-4-(3-(pyridin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C23H18F3N3O2
 1
1 IC50 = 4 nM
CP0036327
7-methyl-4-(3-(3-methylisoxazol-5-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C21H16F3N3O2
 1
1 IC50 = 5 nM
CP0052924
4-(3-(6-methoxypyridin-3-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C23H18F3N3O2
 1
1 IC50 = 5 nM
CP0039555
4-(3-(6-cyclopropylpyridin-3-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C25H20F3N3O
 1
1 IC50 = 6 nM
CP0232347
7-ethoxy-4-(3-(2-methylpyridin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C24H20F3N3O2
 1
1 IC50 = 6 nM
CP0332809
7-methyl-4-(3-(pyrimidin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C21H15F3N4O
 1
1 IC50 = 6 nM
CP0237659
4-(3-(2,6-dimethylpyridin-4-yl)phenyl)-7,8-bis(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C24H17F6N3O
 1
1 IC50 = 7 nM
CP0161928
4-(3-(1H-1,2,4-triazol-1-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C19H14F3N5O
 1
1 IC50 = 8 nM
CP0237661
8-chloro-4-(3-(pyridin-4-yl)phenyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C20H14ClN3O
 1
1 IC50 = 8 nM
CP0295951
4-(3-(2-ethylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C24H20F3N3O
 1
1 IC50 = 8 nM
CP0336098
4-(3-(2-(methoxymethyl)-6-methylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C25H22F3N3O2
 1
1 IC50 = 8 nM
CP0349551
4-(3-(1H-1,2,3-triazol-1-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C19H14F3N5O
 1
1 IC50 = 9 nM
CP0161929
4-(3-(6-ethylpyridin-3-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C24H20F3N3O
 1
1 IC50 = 9 nM
CP0053390
4-(3-(2-cyclopropylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C25H20F3N3O
 1
1 IC50 = 10 nM
CP0053392
4-(3-(6-isopropylpyridin-3-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C25H22F3N3O
 1
1 IC50 = 10 nM
CP0101910
4-(3-(2-cyclopentylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C27H24F3N3O
 1
1 IC50 = 10 nM
CP0237670
4-(3-(pyridin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C21H14F3N3O
 1
1 IC50 = 10 nM
CP0059416
4-(3-(1H-imidazol-1-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C20H15F3N4O
 1
1 IC50 = 12 nM
CP0059417
8-(2-fluorophenyl)-4-(3-imidazol-1-ylphenyl)-1,3-dihydro-1,5-benzodiazepin-2-one
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C24H17FN4O
 1
1 IC50 = 12 nM
CP0162027
4-(3-(1H-1,2,3-triazol-1-yl)phenyl)-8-(2-fluorophenyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C23H16FN5O
 2
1 IC50 = 12 nM
2 IC50 = 16 nM
CP0368814
4-(3-(7-methyl-2-oxo-8-(trifluoromethyl)-2,3-dihydro-1H-benzo[b][1,4]diazepin-4-yl)phenyl)picolinonitrile
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C23H15F3N4O
 1
1 IC50 = 12 nM
CP0038458
4-(3-(2-methoxypyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C23H18F3N3O2
 1
1 IC50 = 13 nM
CP0295952
4-(3-(2-(methoxymethyl)pyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C24H20F3N3O2
 1
1 IC50 = 13 nM
CP0297211
4-(3-(2-(hydroxymethyl)pyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C23H18F3N3O2
 1
1 IC50 = 13 nM
CP0337808
7-methyl-4-(3-(6-methylpyridin-3-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C23H18F3N3O
 1
1 IC50 = 13 nM
CP0237671
4-(3-(6-aminopyridin-3-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C22H17F3N4O
 1
1 IC50 = 14 nM
CP0295953
4-(3-(2-(hydroxymethyl)-6-methylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C24H20F3N3O2
 1
1 IC50 = 14 nM
CP0218960
4-(3-(2-benzylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C29H22F3N3O
 1
1 IC50 = 16 nM
CP0484073
8-(4-fluorophenyl)-4-(3-imidazol-1-ylphenyl)-1,3-dihydro-1,5-benzodiazepin-2-one
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C24H17FN4O
 1
1 IC50 = 17 nM
CP0237672
7-methyl-4-(3-(pyridazin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C21H15F3N4O
 1
1 IC50 = 18 nM
CP0295954
4-(3-(2-methylpyridin-4-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C22H16F3N3O
 1
1 IC50 = 18 nM
CP0283397
7-methyl-4-(3-(pyrazin-2-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C21H15F3N4O
 1
1 IC50 = 20 nM
CP0205609
8-(2-fluorophenyl)-7-hydroxy-4-(3-imidazol-1-ylphenyl)-1,3-dihydro-1,5-benzodiazepin-2-one
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C24H17FN4O2
 1
1 IC50 = 22 nM
CP0336099
7-methyl-4-(3-(6-(pyrimidin-5-yl)pyridin-3-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C21H15F3N4O
 1
1 IC50 = 23 nM
CP0101912
4-(3-(1H-imidazol-1-yl)phenyl)-8-((4-fluorophenyl)ethynyl)-7-hydroxy-1H-benzo[b][1,4]diazepin-2(3H)-one
   Show/Hide
C26H17FN4O2
 1
1 IC50 = 26 nM
CP0295955
4-(3-(2,2'-bipyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C22H16F3N3O
 1
1 IC50 = 26 nM
CP0079531
(E)-3-(4-oxo-7-(2-phenylethynyl)-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)benzonitrile
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C24H15N3O
 1
1 IC50 = 34 nM
CP0243343
4-(3-(1-methyl-1H-pyrazol-5-yl)phenyl)-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C20H15F3N4O
 1
1 IC50 = 39 nM
CP0335052
4-(3-(2-(2-hydroxypropan-2-yl)pyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one
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C25H22F3N3O2
 1
1 IC50 = 40 nM
CP0295902
8-methyl-4-phenyl-1H-benzo[b][1,4]diazepin-2(3H)-one
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C16H14N2O
 1
1 IC50 = 6400 nM