General Information of the Protein
Protein ID
PT01473
Protein Name
Glucagon receptor
Gene Name
GCGR
Sequence
MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNRTFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQCQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANLFASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYCWLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDNMGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGVHEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRLGKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family B G protein-coupled receptor
>
Peptide receptor (family B GPCR)
>
Glucagon-like receptor
>
Glucagon receptor
Function
G-protein coupled receptor for glucagon that plays a central role in the regulation of blood glucose levels and glucose homeostasis. Regulates the rate of hepatic glucose production by promoting glycogen hydrolysis and gluconeogenesis. Plays an important role in mediating the responses to fasting. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Promotes activation of adenylate cyclase. Besides, plays a role in signaling via a phosphatidylinositol-calcium second messenger system.
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Uniprot ID
Primary ID:
P47871

Secondarily ID:
Q2M3M5
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HGNC ID
HGNC:4192
Subcellular Location
Cell membrane
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: CL000051 , BHK-21
Compound ID Compound Name Compound Formula
CP0134277
3-Cyano-4-hydroxy-benzoic acid [1-(2,3,5,6-tetramethyl-benzyl)-1H-indol-4-ylmethylene]-hydrazide
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C28H26N4O2
 1
1
IC50 = 2.3 nM
   TI
   LI
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   TS
CP0910043
Cyclopentanecarboxylic acid {4-[(3-cyano-4-hydroxy-benzoyl)-hydrazonomethyl]-naphthalen-1-yl}-cyclopentanecarbonyl-amide
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C31H30N4O4
 1
1
IC50 = 2.8 nM
   TI
   LI
   LO
   TS
CP0869586
Cyclopentanecarboxylic acid {4-[(3-chloro-4-hydroxy-benzoyl)-hydrazonomethyl]-naphthalen-1-yl}-cyclopentanecarbonyl-amide
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C30H30ClN3O4
 1
1
IC50 = 3.4 nM
   TI
   LI
   LO
   TS
CP0070503
(R)-3-{4-[1-(4-Cyclohex-1-enylphenyl)-3-(3,5-dichlorophenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C30H29Cl2N3O5
 1
1
IC50 = 3.9 nM
   TI
   LI
   LO
   TS
CP0441152
(R)-3-{4-[1-(4-Cyclohexylphenyl)-3-(3,5-dichlorophenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C30H31Cl2N3O5
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0358493
3-Chloro-4-hydroxy-benzoic acid [1-[4-(4-isopropyl-benzyloxy)-naphthalen-1-yl]-meth-(E)-ylidene]-hydrazide
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C28H25ClN2O3
 1
1
IC50 = 4.3 nM
   TI
   LI
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   TS
CP0467464
3-Chloro-4-hydroxy-benzoic acid (4-{2-[4-(4-chloro-benzyl)-piperazin-1-yl]-2-oxo-ethyl}-naphthalen-1-ylmethylene)-hydrazide
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C31H28Cl2N4O3
 1
1
IC50 = 4.6 nM
   TI
   LI
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   TS
CP0492454
3-Cyano-4-hydroxy-benzoic acid {4-[4-(4-chloro-benzyl)-piperazine-1-carbonyl]-naphthalen-1-ylmethylene}-hydrazide
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C31H26ClN5O3
 1
1
IC50 = 4.9 nM
   TI
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   TS
CP0462586
(R)-3-{4-[1-(4-Cyclohex-1-enylphenyl)-3-(3-methanesulfonyl-4-trifluoromethoxyphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C32H32F3N3O8S
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0504622
3-Chloro-4-hydroxy-benzoic acid [1-(2,3,5,6-tetramethyl-benzyl)-1H-indol-4-ylmethylene]-hydrazide
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C27H26ClN3O2
 1
1
IC50 = 5.3 nM
   TI
   LI
   LO
   TS
CP0497587
3-Chloro-4-hydroxy-benzoic acid [1-(2,4,6-trimethyl-benzyl)-1H-indol-4-ylmethylene]-hydrazide
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C26H24ClN3O2
 1
1
IC50 = 5.8 nM
   TI
   LI
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   TS
CP0437619
4-[(3-Chloro-4-hydroxy-benzoyl)-hydrazonomethyl]-naphthalene-1-carboxylic acid [2-(4-chloro-phenyl)-ethyl]-amide
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C27H21Cl2N3O3
 1
1
IC50 = 5.9 nM
   TI
   LI
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   TS
CP0463788
(R)-3-{4-[1-(4-Cyclohexylphenyl)-3-(4-trifluoromethylsulfanylphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C31H32F3N3O5S
 1
1
IC50 = 6 nM
   TI
   LI
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   TS
CP0503148
(R)-3-{4-[1-(4-Cyclohex-1-enylphenyl)-3-(2,2,4,4-tetrafluoro-4H-benzo[1,3]dioxin-6-yl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C32H29F4N3O7
 1
1
IC50 = 6 nM
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CP0464831
3-Cyano-4-hydroxy-benzoic acid (4-{2-[4-(4-bromo-phenyl)-3,6-dihydro-2H-pyridin-1-yl]-2-oxo-ethoxy}-naphthalen-1-ylmethylene)-hydrazide
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C32H25BrN4O4
 1
1
IC50 = 6.1 nM
   TI
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CP0527656
N-[(E)-[4-[2-[benzyl-[2-(dimethylamino)ethyl]amino]-2-oxoethyl]naphthalen-1-yl]methylideneamino]-3-chloro-4-hydroxybenzamide
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C31H31ClN4O3
 1
1
IC50 = 6.2 nM
   TI
   LI
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CP0462323
3-cyano-N-[(E)-[1-(2-cyclopentylacetyl)indol-3-yl]methylideneamino]-4-hydroxybenzamide
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C24H22N4O3
 1
1
IC50 = 6.4 nM
   TI
   LI
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CP0508894
3-Chloro-4-hydroxy-benzoic acid (4-{2-[4-(4-bromo-phenyl)-3,6-dihydro-2H-pyridin-1-yl]-2-oxo-ethoxy}-naphthalen-1-ylmethylene)-hydrazide
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C31H25BrClN3O4
 1
1
IC50 = 6.6 nM
   TI
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CP0515732
3-chloro-4-hydroxy-N-[(E)-[4-[[4-(trifluoromethoxy)phenyl]methylsulfonylmethyl]naphthalen-1-yl]methylideneamino]benzamide
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C27H20ClF3N2O5S
 1
1
IC50 = 6.9 nM
   TI
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CP0459788
(R)-3-{4-[3-(3-Bromo-5-trifluoromethylphenyl)-1-(4-cyclohex-1-enylphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C31H29BrF3N3O5
 1
1
IC50 = 7 nM
   TI
   LI
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   TS
CP0391322
3-Chloro-4-hydroxy-benzoic acid {4-[2-(2-ethyl-piperidin-1-yl)-2-oxo-ethyl]-naphthalen-1-ylmethylene}-hydrazide
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C27H28ClN3O3
 1
1
IC50 = 7.4 nM
   TI
   LI
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CP0497915
N-[(E)-[4-[[(2R)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]naphthalen-1-yl]methylideneamino]-3-chloro-4-hydroxybenzamide
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C27H23ClN4O3
 1
1
IC50 = 7.4 nM
   TI
   LI
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CP0436745
3-Chloro-4-hydroxy-benzoic acid (4-{2-[4-(2-fluoro-phenyl)-piperazin-1-yl]-2-oxo-ethyl}-naphthalen-1-ylmethylene)-hydrazide
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C30H26ClFN4O3
 1
1
IC50 = 7.9 nM
   TI
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CP0383869
(R)-trans-3-{4-[3-(3,5-Bis(trifluoromethyl)phenyl)-1-(4-tert-butylcyclohexyl)ureidomethyl]-benzoylamino}-2-hydroxypropionic acid
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C30H35F6N3O5
 1
1
IC50 = 8 nM
   TI
   LI
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CP0459789
(R)-3-{4-[3-(3-Bromophenyl)-1-(4-cyclohexylphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C30H32BrN3O5
 1
1
IC50 = 8 nM
   TI
   LI
   LO
   TS
CP0431401
3-Chloro-4-hydroxy-benzoic acid {4-[2-(2-methyl-piperidin-1-yl)-2-oxo-ethyl]-naphthalen-1-ylmethylene}-hydrazide
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C26H26ClN3O3
 1
1
IC50 = 8.3 nM
   TI
   LI
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   TS
CP0527654
3-Chloro-4-hydroxy-benzoic acid [4-(4-chloro-benzylamino)-naphthalen-1-ylmethylene]-hydrazide
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C25H19Cl2N3O2
 1
1
IC50 = 8.3 nM
   TI
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CP0435018
(R)-3-{4-[1-(4-Cyclohexylphenyl)-3-(3-methylthio)phenyl-ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C31H35N3O5S
 1
1
IC50 = 9 nM
   TI
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CP0497971
(R)-3-{4-[1-(4-Cyclohexylphenyl)-3-(3-methoxy-5-trifluoromethylphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionicacid
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C32H34F3N3O6
 1
1
IC50 = 9 nM
   TI
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CP0517419
(R)-3-{4-[3-(4-Cyano-3-trifluoromethylphenyl)-1-(4-cyclohexylphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C32H31F3N4O5
 1
1
IC50 = 9 nM
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   LI
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CP0432380
3-Chloro-4-hydroxy-benzoic acid {4-[2-(4-benzyl-piperazin-1-yl)-2-oxo-ethyl]-naphthalen-1-ylmethylene}-hydrazide
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C31H29ClN4O3
 1
1
IC50 = 9.2 nM
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CP0423784
(R)-trans-3-{4-[1-(4-tert-Butyl-cyclohexyl)-3-(3-methyl-5-trifluoromethylphenyl)ureidomethyl]benzoylamino}-2-hydroxy-propionic acid
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C30H38F3N3O5
 1
1
IC50 = 10 nM
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CP0474597
N-[(E)-[4-[2-[benzyl-[2-(dimethylamino)ethyl]amino]-2-oxoethyl]naphthalen-1-yl]methylideneamino]-3-cyano-4-hydroxybenzamide
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C32H31N5O3
 1
1
IC50 = 10.4 nM
   TI
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CP0508907
3-Chloro-4-hydroxy-benzoic acid {4-[4-(4-chloro-benzyl)-piperazine-1-carbonyl]-naphthalen-1-ylmethylene}-hydrazide
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C30H26Cl2N4O3
 1
1
IC50 = 11.3 nM
   TI
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CP0492544
3-Chloro-4-hydroxy-benzoic acid (4-{2-[4-(4-bromo-phenyl)-4-hydroxy-piperidin-1-yl]-2-oxo-ethoxy}-naphthalen-1-ylmethylene)-hydrazide
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C31H27BrClN3O5
 1
1
IC50 = 11.4 nM
   TI
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CP0404471
3-Cyano-4-hydroxy-benzoic acid {4-[2-(2-methyl-piperidin-1-yl)-2-oxo-ethyl]-naphthalen-1-ylmethylene}-hydrazide
   Show/Hide
C27H26N4O3
 1
1
IC50 = 11.6 nM
   TI
   LI
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CP0211346
3-(4-((1-(4-cyclohexenylphenyl)-3-(3,5-dichlorophenyl)ureido)methyl)benzamido)propanoic acid
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C30H29Cl2N3O4
 2
1
IC50 = 12 nM
   TI
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2
IC50 = 27 nM
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CP0565416
3-Chloro-4-hydroxy-benzoic acid (4-{2-[4-(4-fluoro-phenyl)-piperazin-1-yl]-2-oxo-ethyl}-naphthalen-1-ylmethylene)-hydrazide
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C30H26ClFN4O3
 1
1
IC50 = 12.3 nM
   TI
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CP0430977
3-chloro-4-hydroxy-N-[(E)-[5-[[4-(trifluoromethoxy)phenyl]methoxy]naphthalen-1-yl]methylideneamino]benzamide
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C26H18ClF3N2O4
 1
1
IC50 = 12.9 nM
   TI
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CP0375059
(R)-3-{4-[1-(4-Cyclohex-1-enylphenyl)-3-(3-fluoro-5-trifluoromethylphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C31H29F4N3O5
 1
1
IC50 = 13 nM
   TI
   LI
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CP0497916
3-Chloro-4-hydroxy-benzoic acid {4-[2-(3,4-dihydro-1H-isoquinolin-2-yl)-2-oxo-ethoxy]-naphthalen-1-ylmethylene}-hydrazide
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C29H24ClN3O4
 1
1
IC50 = 13.8 nM
   TI
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CP0375060
(R)-3-{4-[3-(3-Chlorophenyl)-1-(4-cyclohex-1-enylphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C30H30ClN3O5
 1
1
IC50 = 14 nM
   TI
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CP0423783
(R/S)-3-{4-[1-(4-Cyclohex-1-enylphenyl)-3-(3,5-dichlorophenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C30H29Cl2N3O5
 1
1
IC50 = 14 nM
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CP0454980
(R)-3-{4-[1-(4-Cyclohex-1-enylphenyl)-3-(3-methoxy-5-trifluoromethylphenyl)ureidomethyl]-benzoylamino}-2-hydroxypropionic acid
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C32H32F3N3O6
 1
1
IC50 = 14 nM
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CP0503427
3-chloro-4-hydroxy-N-[(E)-[2-methoxy-4-[[2-[4-(trifluoromethoxy)phenyl]sulfanylacetyl]amino]phenyl]methylideneamino]benzamide
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C24H19ClF3N3O5S
 1
1
IC50 = 14.5 nM
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CP0494732
3-Chloro-4-hydroxy-benzoic acid {4-[2-(3,4-dichloro-benzylamino)-ethoxy]-naphthalen-1-ylmethylene}-hydrazide
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C27H22Cl3N3O3
 1
1
IC50 = 14.7 nM
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CP0492455
3-cyano-4-hydroxy-N-[(E)-[2-methoxy-4-[3-[4-(trifluoromethyl)phenyl]propanoylamino]phenyl]methylideneamino]benzamide
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C26H21F3N4O4
 1
1
IC50 = 15.7 nM
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CP0430821
3-[[4-[[[3,5-bis(trifluoromethyl)phenyl]carbamoyl-(4-tert-butylcyclohexyl)amino]methyl]benzoyl]amino]propanoic acid
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C30H35F6N3O4
 2
1
IC50 = 16 nM
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2
IC50 = 56 nM
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CP0516016
2-{4-[(3-Cyano-4-hydroxy-benzoyl)-hydrazonomethyl]-naphthalen-1-yl}-N,N-diethyl-acetamide
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C25H24N4O3
 1
1
IC50 = 16.5 nM
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CP0459787
(R)-3-{4-[3-(3-tert-Butylphenyl)-1-(4-cyclohexylphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C34H41N3O5
 1
1
IC50 = 18 nM
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CP0431442
3-cyano-N-[(E)-[1-[4-(dimethylamino)benzoyl]indol-3-yl]methylideneamino]-4-hydroxybenzamide
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C26H21N5O3
 1
1
IC50 = 19.1 nM
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CP0500229
3-Chloro-4-hydroxy-benzoic acid (4-{2-[2-(4-bromo-phenyl)-ethylamino]-ethoxy}-naphthalen-1-ylmethylene)-hydrazide
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C28H25BrClN3O3
 1
1
IC50 = 19.7 nM
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CP0045459
3-Cyano-4-hydroxy-benzoic acid [1-[4-(4-isopropyl-benzyloxy)-3,5-dimethoxy-phenyl]-meth-(E)-ylidene]-hydrazide
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C27H27N3O5
 1
1
IC50 = 20 nM
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CP0919228
N-{4-[(3-Chloro-4-hydroxy-benzoyl)-hydrazonomethyl]-3-methoxy-phenyl}-3-(4-trifluoromethyl-phenyl)-propionamide
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C25H23ClF3N3O5
 1
1
IC50 = 21.2 nM
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CP0408083
3-Cyano-4-hydroxy-benzoic acid [1-(4-trifluoromethyl-benzyl)-1H-indol-4-ylmethylene]-hydrazide
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C25H17F3N4O2
 1
1
IC50 = 22.3 nM
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CP0430978
2-{4-[(3-Chloro-4-hydroxy-benzoyl)-hydrazonomethyl]-naphthalen-1-yl}-N,N-diethyl-acetamide
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C24H24ClN3O3
 1
1
IC50 = 22.6 nM
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CP0492624
3-Chloro-4-hydroxy-benzoic acid [1-(4-trifluoromethoxy-benzyl)-1H-indol-4-ylmethylene]-hydrazide
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C24H17ClF3N3O3
 1
1
IC50 = 22.9 nM
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CP0269118
3-Chloro-4-hydroxy-benzoic acid [1-(4-isopropyl-benzyl)-1H-indol-4-ylmethylene]-hydrazide
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C26H24ClN3O2
 1
1
IC50 = 23 nM
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CP0435017
3-(4-((1-(4-tert-butylcyclohexyl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)benzamido)propanoic acid
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C29H36F3N3O5
 1
1
IC50 = 23.4 nM
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CP0475022
thiazole, 28
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C28H22ClF3N2O4S
 2
1
IC50 = 25 nM
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2
IC50 = 153 nM
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CP0387508
(R)-trans-3-{4-[1-(4-tert-Butylcyclohexyl)-3-(3,5-dimethylphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C30H41N3O5
 1
1
IC50 = 27 nM
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CP0463735
3-Chloro-4-hydroxy-benzoic acid [1-(3,4-dichloro-benzyl)-1H-indol-4-ylmethylene]-hydrazide
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C23H16Cl3N3O2
 1
1
IC50 = 27.5 nM
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CP0471839
3-Chloro-4-hydroxy-benzoic acid {4-[2-(4-trifluoromethoxy-benzylamino)-ethoxy]-naphthalen-1-ylmethylene}-hydrazide
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C28H23ClF3N3O4
 1
1
IC50 = 27.7 nM
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CP0492322
2-(4-Chloro-phenyl)-N-{4-[(3-cyano-4-hydroxy-benzoyl)-hydrazonomethyl]-3-methoxy-phenyl}-acetamide
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C24H19ClN4O4
 1
1
IC50 = 28.7 nM
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CP0492305
3-Fluoro-4-hydroxy-benzoic acid (4-hydroxymethyl-naphthalen-1-ylmethylene)-hydrazide
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C19H15FN2O3
 1
1
IC50 = 29.4 nM
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CP0492289
3-Cyano-4-hydroxy-benzoic acid (4-hydroxymethyl-naphthalen-1-ylmethylene)-hydrazide
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C20H15N3O3
 1
1
IC50 = 29.8 nM
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CP0502489
3-chloro-N-[(E)-[4-(2,2-dimethylpropanoylamino)naphthalen-1-yl]methylideneamino]-4-hydroxybenzamide
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C23H22ClN3O3
 1
1
IC50 = 33 nM
   TI
   LI
   LO
   TS
CP0432456
3-chloro-4-hydroxy-N-[(E)-[2-methoxy-4-[3-[4-(trifluoromethyl)phenyl]propanoylamino]phenyl]methylideneamino]benzamide
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C25H21ClF3N3O4
 1
1
IC50 = 33.5 nM
   TI
   LI
   LO
   TS
CP0483803
3-Chloro-4-hydroxy-benzoic acid [1-(4-trifluoromethyl-benzyl)-1H-indol-4-ylmethylene]-hydrazide
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C24H17ClF3N3O2
 1
1
IC50 = 33.8 nM
   TI
   LI
   LO
   TS
CP0374454
aminothiazole, 21
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C28H21F6N3O3S2
 1
1
IC50 = 34 nM
   TI
   LI
   LO
   TS
CP0374455
aminothiazole, 24
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C33H26ClN3O3S
 2
1
IC50 = 34 nM
   TI
   LI
   LO
   TS
2
IC50 = 93 nM
   TI
   LI
   LO
   TS
CP0502729
3-(4-((1-(4-tert-butylcyclohexyl)-3-(4-isopropylphenyl)ureido)methyl)benzamido)propanoic acid
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C31H43N3O4
 1
1
IC50 = 35 nM
   TI
   LI
   LO
   TS
CP0497661
4-[(3-Chloro-4-hydroxy-benzoyl)-hydrazonomethyl]-naphthalene-1-carboxylic acid diethylamide
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C23H22ClN3O3
 1
1
IC50 = 35.4 nM
   TI
   LI
   LO
   TS
CP0443414
aminothiazole, 3
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C33H30F3N3O4S
 1
1
IC50 = 36 nM
   TI
   LI
   LO
   TS
CP0500823
3-{4-[1-(4-tert-Butylphenyl)-3-(4-trifluoromethoxyphenyl)ureidomethyl]benzoylamino}propionicacid
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C29H30F3N3O5
 2
1
IC50 = 36 nM
   TI
   LI
   LO
   TS
2
IC50 = 96 nM
   TI
   LI
   LO
   TS
CP0374456
thiazole, 27
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C28H22ClF3N2O3S
 2
1
IC50 = 38 nM
   TI
   LI
   LO
   TS
2
IC50 = 96 nM
   TI
   LI
   LO
   TS
CP0492319
3-chloro-N-[(E)-[4-(cyclopentanecarbonylamino)naphthalen-1-yl]methylideneamino]-4-hydroxybenzamide
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C24H22ClN3O3
 1
1
IC50 = 38.8 nM
   TI
   LI
   LO
   TS
CP0535009
3-Chloro-4-hydroxy-benzoic acid (4-hydroxymethyl-naphthalen-1-ylmethylene)-hydrazide
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C19H15ClN2O3
 1
1
IC50 = 41.1 nM
   TI
   LI
   LO
   TS
CP0538146
3-[[4-[[(4-tert-butylcyclohexyl)-[[4-(trifluoromethoxy)phenyl]carbamoyl]amino]methyl]benzoyl]amino]propanoic acid
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C29H36F3N3O5
 1
1
IC50 = 47 nM
   TI
   LI
   LO
   TS
CP0522589
3-cyano-4-hydroxy-N-[(E)-[2-methoxy-4-[[2-[3-(trifluoromethyl)phenyl]acetyl]amino]phenyl]methylideneamino]benzamide
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C25H19F3N4O4
 1
1
IC50 = 47.8 nM
   TI
   LI
   LO
   TS
CP0475018
aminothiazole, 4
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C33H30F3N3O3S
 1
1
IC50 = 48 nM
   TI
   LI
   LO
   TS
CP0443415
aminothiazole, 11
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C31H28F3N3O3S
 2
1
IC50 = 48 nM
   TI
   LI
   LO
   TS
2
IC50 = 77 nM
   TI
   LI
   LO
   TS
CP0362260
2-{4-[(3-Chloro-4-hydroxy-benzoyl)-hydrazonomethyl]-naphthalen-1-yloxy}-N,N-diethyl-acetamide
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C24H24ClN3O4
 1
1
IC50 = 49.7 nM
   TI
   LI
   LO
   TS
CP0443411
aminothiazole, 6
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C34H26F3N3O4S
 2
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
2
IC50 = 59 nM
   TI
   LI
   LO
   TS
CP0468561
aminothiazole, 19
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C28H21F6N3O4S
 2
1
IC50 = 51 nM
   TI
   LI
   LO
   TS
2
IC50 = 92 nM
   TI
   LI
   LO
   TS
CP0466540
(S)-3-{4-[1-(4-Cyclohex-1-enylphenyl)-3-(3,5-dichlorophenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C30H29Cl2N3O5
 1
1
IC50 = 51 nM
   TI
   LI
   LO
   TS
CP0492190
2-{4-[(3-Chloro-4-hydroxy-benzoyl)-hydrazonomethyl]-naphthalen-1-yloxy}-N-(4-chloro-phenyl)-acetamide
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C26H19Cl2N3O4
 1
1
IC50 = 51.7 nM
   TI
   LI
   LO
   TS
CP0443416
aminothiazole, 17
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C27H21ClF3N3O4S
 2
1
IC50 = 53 nM
   TI
   LI
   LO
   TS
2
IC50 = 82 nM
   TI
   LI
   LO
   TS
CP0475021
aminothiazole, 16
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C27H21ClF3N3O3S
 2
1
IC50 = 53 nM
   TI
   LI
   LO
   TS
2
IC50 = 76 nM
   TI
   LI
   LO
   TS
CP0492316
2,3-Dichloro-4-hydroxy-benzoic acid (4-hydroxymethyl-naphthalen-1-ylmethylene)-hydrazide
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C19H14Cl2N2O3
 1
1
IC50 = 53.8 nM
   TI
   LI
   LO
   TS
CP0374482
aminothiazole, 10
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C30H27Cl2N3O3S
 2
1
IC50 = 54 nM
   TI
   LI
   LO
   TS
2
IC50 = 79 nM
   TI
   LI
   LO
   TS
CP0514590
3-Chloro-4-hydroxy-benzoic acid {4-[2-(2-trifluoromethoxy-benzylamino)-ethoxy]-naphthalen-1-ylmethylene}-hydrazide
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C28H23ClF3N3O4
 1
1
IC50 = 54.3 nM
   TI
   LI
   LO
   TS
CP0047783
3-{4-[1-(4-tert-Butyl-cyclohexyl)-3-(4-trifluoromethoxy-phenyl)-ureidomethyl]-benzoylamino}-propionic acid
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C29H36F3N3O5
 1
1
IC50 = 55 nM
   TI
   LI
   LO
   TS
CP0462530
(R/S)-3-{4-[1-(4-tert-Butylphenyl)-3-(4-trifluoromethoxyphenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C29H30F3N3O6
 1
1
IC50 = 55 nM
   TI
   LI
   LO
   TS
CP0553738
3-[[4-[[(4-tert-butylcyclohexyl)-[[2-cyano-4-(trifluoromethoxy)phenyl]carbamoyl]amino]methyl]benzoyl]amino]propanoic acid
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C30H35F3N4O5
 1
1
IC50 = 56 nM
   TI
   LI
   LO
   TS
CP0538145
3-(4-((1-(4-isopropylcyclohexyl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)benzamido)propanoic acid
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C28H34F3N3O5
 1
1
IC50 = 59 nM
   TI
   LI
   LO
   TS
CP0526964
3-(4-((1-(4-cyclohexylphenyl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)benzamido)propanoic acid
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C31H32F3N3O5
 1
1
IC50 = 61 nM
   TI
   LI
   LO
   TS
CP0480507
N-[(E)-[4-[[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]methyl]naphthalen-1-yl]methylideneamino]-3-chloro-4-hydroxybenzamide
   Show/Hide
C28H25ClN4O3
 1
1
IC50 = 61.8 nM
   TI
   LI
   LO
   TS
CP0462325
2-Benzo[b]thiophen-3-yl-N-{4-[(3-chloro-4-hydroxy-benzoyl)-hydrazonomethyl]-2-methoxy-phenyl}-acetamide
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C25H20ClN3O4S
 1
1
IC50 = 63.2 nM
   TI
   LI
   LO
   TS
CP0494615
aminothiazole, 7
   Show/Hide
C30H26F3N3O3S
 2
1
IC50 = 64 nM
   TI
   LI
   LO
   TS
2
IC50 = 86 nM
   TI
   LI
   LO
   TS
CP0437677
3-chloro-4-hydroxy-N-[(E)-[3-methoxy-4-[[2-[4-(trifluoromethoxy)phenoxy]acetyl]amino]phenyl]methylideneamino]benzamide
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C24H19ClF3N3O6
 1
1
IC50 = 73 nM
   TI
   LI
   LO
   TS
CP0497648
3-chloro-4-hydroxy-N-[(E)-[4-(methoxymethyl)naphthalen-1-yl]methylideneamino]benzamide
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C20H17ClN2O3
 1
1
IC50 = 75.5 nM
   TI
   LI
   LO
   TS
CP0495975
aminothiazole, 25
   Show/Hide
C34H26F3N3O3S
 1
1
IC50 = 78 nM
   TI
   LI
   LO
   TS
CP0495984
3-[[4-[[(4-tert-butylcyclohexyl)-[(3,5-dichlorophenyl)carbamoyl]amino]methyl]benzoyl]amino]propanoic acid
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C28H35Cl2N3O4
 1
1
IC50 = 80 nM
   TI
   LI
   LO
   TS
CP0445398
aminothiazole, 26
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C34H26F3N3O4S
 1
1
IC50 = 81 nM
   TI
   LI
   LO
   TS
CP0497970
(S)-trans-3-{4-[3-(3,5-Bis(trifluoromethyl)phenyl)-1-(4-tert-butylcyclohexyl)ureidomethyl]-benzoylamino}-2-hydroxypropionic acid
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C30H35F6N3O5
 1
1
IC50 = 82 nM
   TI
   LI
   LO
   TS
CP0443417
aminothiazole, 8
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C30H26F3N3O4S
 2
1
IC50 = 85 nM
   TI
   LI
   LO
   TS
2
IC50 = 96 nM
   TI
   LI
   LO
   TS
CP0374468
aminothiazole, 5
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C38H34ClN3O3S
 1
1
IC50 = 86 nM
   TI
   LI
   LO
   TS
CP0404531
N-[(E)-[4-[2-[(1-benzylpyrrolidin-3-yl)amino]-2-oxoethoxy]naphthalen-1-yl]methylideneamino]-3-chloro-4-hydroxybenzamide
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C31H29ClN4O4
 1
1
IC50 = 89.3 nM
   TI
   LI
   LO
   TS
CP0383071
5-Methoxy-benzofuran-2-carboxylic acid {4-[(3-chloro-4-hydroxy-benzoyl)-hydrazonomethyl]-3-methoxy-phenyl}-amide
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C25H20ClN3O6
 1
1
IC50 = 90.6 nM
   TI
   LI
   LO
   TS
CP0468560
aminothiazole, 18
   Show/Hide
C27H21ClF3N3O3S
 2
1
IC50 = 92 nM
   TI
   LI
   LO
   TS
2
IC50 = 93 nM
   TI
   LI
   LO
   TS
CP0443412
aminothiazole, 12
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C31H30F3N3O3S
 2
1
IC50 = 93 nM
   TI
   LI
   LO
   TS
2
IC50 = 119 nM
   TI
   LI
   LO
   TS
CP0434378
3-Chloro-4-hydroxy-benzoic acid {4-[4-(4-chloro-benzyl)-piperazin-1-ylmethyl]-naphthalen-1-ylmethylene}-hydrazide
   Show/Hide
C30H28Cl2N4O2
 1
1
IC50 = 96.7 nM
   TI
   LI
   LO
   TS
CP0494614
thiazole, 29
   Show/Hide
C28H22ClF3N2O4S
 1
1
IC50 = 98 nM
   TI
   LI
   LO
   TS
CP0485224
aminothiazole, 9
   Show/Hide
C29H25Cl2N3O3S
 1
1
IC50 = 99 nM
   TI
   LI
   LO
   TS
CP0377320
3-(4-{[N-(5-chlorobenzo[b]thiophen-3-carbonyl)-N-(2,2-diphenylethyl)amino]methyl}benzoylamino)propionic acid
   Show/Hide
C33H27ClN2O4S
 1
1
IC50 = 116 nM
   TI
   LI
   LO
   TS
CP0485223
aminothiazole, 2
   Show/Hide
C36H39N3O3S
 1
1
IC50 = 118 nM
   TI
   LI
   LO
   TS
CP0495973
thiazole, 30
   Show/Hide
C29H22F6N2O5S
 1
1
IC50 = 119 nM
   TI
   LI
   LO
   TS
CP0392904
3-Chloro-4-hydroxy-benzoic acid {4-[2-(3,4-dihydro-1H-isoquinolin-2-yl)-ethoxy]-2-methoxy-benzylidene}-hydrazide
   Show/Hide
C26H26ClN3O4
 1
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
CP0523167
3-{4-[1-(4-propylcyclohexyl)-3-(4-trifluoromethoxyphenyl)ureidomethyl]benzoylamino}propionic acid
   Show/Hide
C28H34F3N3O5
 1
1
IC50 = 122 nM
   TI
   LI
   LO
   TS
CP0435234
aminothiazole, 1
   Show/Hide
C32H31N3O3S
 1
1
IC50 = 130 nM
   TI
   LI
   LO
   TS
CP0374471
aminothiazole, 13
   Show/Hide
C32H29F6N3O3S
 1
1
IC50 = 131 nM
   TI
   LI
   LO
   TS
CP0467361
3-Chloro-4-hydroxy-benzoic acid {2-methoxy-4-[2-(4-trifluoromethyl-benzylamino)-ethoxy]-benzylidene}-hydrazide
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C25H23ClF3N3O4
 1
1
IC50 = 133 nM
   TI
   LI
   LO
   TS
CP0386530
3-(4-((1-(4,4-dipropylcyclohexyl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)benzamido)propanoic acid
   Show/Hide
C31H40F3N3O5
 1
1
IC50 = 137 nM
   TI
   LI
   LO
   TS
CP0528569
3-[[4-[[(4-tert-butylcyclohexyl)-[[4-(cyclopropylmethoxy)phenyl]carbamoyl]amino]methyl]benzoyl]amino]propanoic acid
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C32H43N3O5
 1
1
IC50 = 140 nM
   TI
   LI
   LO
   TS
CP0428129
3-(4-((1-(heptan-3-yl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)benzamido)propanoic acid
   Show/Hide
C26H32F3N3O5
 1
1
IC50 = 141 nM
   TI
   LI
   LO
   TS
CP0377323
3-[[4-[[[2-bromo-4-(trifluoromethoxy)phenyl]carbamoyl-(4-tert-butylcyclohexyl)amino]methyl]benzoyl]amino]propanoic acid
   Show/Hide
C29H35BrF3N3O5
 1
1
IC50 = 153 nM
   TI
   LI
   LO
   TS
CP0461108
3-cyano-4-hydroxy-N-[(E)-[4-(propan-2-ylsulfonylmethyl)naphthalen-1-yl]methylideneamino]benzamide
   Show/Hide
C23H21N3O4S
 1
1
IC50 = 163 nM
   TI
   LI
   LO
   TS
CP0375061
(R)-3-{4-[1-(4-Cyclohex-1-enylphenyl)-3-phenyl-ureidomethyl]benzoylamino}-2-hydroxypropionic acid
   Show/Hide
C30H31N3O5
 1
1
IC50 = 166 nM
   TI
   LI
   LO
   TS
CP0495983
3-(4-((1-(4-cyclohexylphenyl)-3-(3-nitrophenyl)ureido)methyl)benzamido)propanoic acid
   Show/Hide
C30H32N4O6
 1
1
IC50 = 167 nM
   TI
   LI
   LO
   TS
CP0537914
3-(4-((3-(4-butylphenyl)-1-(2,3-dihydro-1H-inden-2-yl)ureido)methyl)benzamido)propanoic acid
   Show/Hide
C31H35N3O4
 1
1
IC50 = 179 nM
   TI
   LI
   LO
   TS
CP0457258
3-Chloro-4-hydroxy-benzoic acid [4-(2-methyl-propane-1-sulfonyl)-naphthalen-1-ylmethylene]-hydrazide
   Show/Hide
C22H21ClN2O4S
 1
1
IC50 = 181 nM
   TI
   LI
   LO
   TS
CP0553739
3-[[4-[[(4-tert-butylcyclohexyl)-[[4-(cyclopropylmethoxy)-2-(trifluoromethyl)phenyl]carbamoyl]amino]methyl]benzoyl]amino]propanoic acid
   Show/Hide
C33H42F3N3O5
 1
1
IC50 = 182 nM
   TI
   LI
   LO
   TS
CP0448297
3-Chloro-4-hydroxy-benzoic acid (5-hydroxymethyl-naphthalen-1-ylmethylene)-hydrazide
   Show/Hide
C19H15ClN2O3
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0129520
3-Chloro-4-hydroxy-benzoic acid (4-hydroxy-naphthalen-1-ylmethylene)-hydrazide
   Show/Hide
C18H13ClN2O3
 1
1
IC50 = 203 nM
   TI
   LI
   LO
   TS
CP0419621
3-[[4-[[(4-tert-butylcyclohexyl)-[[4-cyano-2-(trifluoromethoxy)phenyl]carbamoyl]amino]methyl]benzoyl]amino]propanoic acid
   Show/Hide
C30H35F3N4O5
 1
1
IC50 = 215 nM
   TI
   LI
   LO
   TS
CP0462046
3-chloro-N-[(E)-[4-(cyclopentylsulfonylmethyl)naphthalen-1-yl]methylideneamino]-4-hydroxybenzamide
   Show/Hide
C24H23ClN2O4S
 1
1
IC50 = 221 nM
   TI
   LI
   LO
   TS
CP0495972
aminothiazole, 22
   Show/Hide
C30H26F3N3O5S
 1
1
IC50 = 225 nM
   TI
   LI
   LO
   TS
CP0518067
3-[[4-[[(4-tert-butylcyclohexyl)-[(3,4-dichlorophenyl)carbamoyl]amino]methyl]benzoyl]amino]propanoic acid
   Show/Hide
C28H35Cl2N3O4
 1
1
IC50 = 226 nM
   TI
   LI
   LO
   TS
CP0485225
aminothiazole, 23
   Show/Hide
C30H26F3N3O4S
 1
1
IC50 = 261 nM
   TI
   LI
   LO
   TS
CP0529681
3-(4-((1-(2,3-dihydro-1H-inden-2-yl)-3-(4-(trifluoromethylthio)phenyl)ureido)methyl)benzamido)propanoic acid
   Show/Hide
C28H26F3N3O4S
 1
1
IC50 = 262 nM
   TI
   LI
   LO
   TS
CP0414828
3-Chloro-4-hydroxy-benzoic acid {4-[2-(4-methyl-piperazin-1-yl)-2-oxo-ethyl]-naphthalen-1-ylmethylene}-hydrazide
   Show/Hide
C25H25ClN4O3
 1
1
IC50 = 268 nM
   TI
   LI
   LO
   TS
CP0425328
3-Chloro-4-hydroxy-benzoic acid [1-(4-trifluoromethoxy-benzyl)-1H-indol-5-ylmethylene]-hydrazide
   Show/Hide
C24H17ClF3N3O3
 1
1
IC50 = 286 nM
   TI
   LI
   LO
   TS
CP0466338
3-Chloro-4-hydroxy-benzoic acid [1-(4-difluoromethoxy-benzyl)-1H-indol-3-ylmethylene]-hydrazide
   Show/Hide
C24H18ClF2N3O3
 1
1
IC50 = 305 nM
   TI
   LI
   LO
   TS
CP0547270
aminothiazole, 14
   Show/Hide
C34H39N3O3S
 1
1
IC50 = 315 nM
   TI
   LI
   LO
   TS
CP0463061
3-Chloro-4-hydroxy-benzoic acid [4-(propane-2-sulfonyl)-naphthalen-1-ylmethylene]-hydrazide
   Show/Hide
C21H19ClN2O4S
 1
1
IC50 = 357 nM
   TI
   LI
   LO
   TS
CP0443413
aminothiazole, 20
   Show/Hide
C28H24F3N3O4S2
 1
1
IC50 = 420 nM
   TI
   LI
   LO
   TS
CP0559933
2-{4-[(3-Chloro-4-hydroxy-benzoyl)-hydrazonomethyl]-naphthalen-1-yl}-N-(2-dimethylamino-ethyl)-N-methyl-acetamide
   Show/Hide
C25H27ClN4O3
 1
1
IC50 = 441 nM
   TI
   LI
   LO
   TS
CP0415392
3-Chloro-4-hydroxy-benzoic acid {3-chloro-4-[2-(3,4-dihydro-1H-isoquinolin-2-yl)-ethoxy]-5-methoxy-benzylidene}-hydrazide
   Show/Hide
C26H25Cl2N3O4
 1
1
IC50 = 485 nM
   TI
   LI
   LO
   TS
CP0528568
3-(4-((1-(4-phenoxycyclohexyl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)benzamido)propanoic acid
   Show/Hide
C31H32F3N3O6
 1
1
IC50 = 528 nM
   TI
   LI
   LO
   TS
CP0445452
aminothiazole, 15
   Show/Hide
C30H27Cl2N3O3S
 1
1
IC50 = 531 nM
   TI
   LI
   LO
   TS
CP0436887
3-(4-((1-(4-cyclopropylidenecyclohexyl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)benzamido)propanoic acid
   Show/Hide
C28H30F3N3O5
 1
1
IC50 = 571 nM
   TI
   LI
   LO
   TS
CP0469272
3-Chloro-4-hydroxy-benzoic acid (1-benzyl-1H-indol-3-ylmethylene)-hydrazide
   Show/Hide
C23H18ClN3O2
 1
1
IC50 = 615 nM
   TI
   LI
   LO
   TS
CP0423785
(R)-3-{4-[1-(4-Cyclohex-1-enylphenyl)-3-(3,5-dichlorophenyl)ureidomethyl]benzoylamino}-2-methoxypropionic acid
   Show/Hide
C31H31Cl2N3O5
 1
1
IC50 = 693 nM
   TI
   LI
   LO
   TS
CP0518066
3-(4-((1-(4-(diethylcarbamoyl)cyclohexyl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)benzamido)propanoic acid
   Show/Hide
C30H37F3N4O6
 1
1
IC50 = 782 nM
   TI
   LI
   LO
   TS
CP0502727
1-(4-((1-(4-tert-butylcyclohexyl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)benzoyl)piperidine-3-carboxylic acid
   Show/Hide
C32H40F3N3O5
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0518069
3-[[4-[[(4-tert-butylcyclohexyl)-[(4-cyanophenyl)carbamoyl]amino]methyl]benzoyl]amino]propanoic acid
   Show/Hide
C29H36N4O4
 1
1
IC50 = 1045 nM
   TI
   LI
   LO
   TS
CP0502728
3-[[4-[[(4-tert-butylcyclohexyl)-(phenylcarbamoyl)amino]methyl]benzoyl]amino]propanoic acid
   Show/Hide
C28H37N3O4
 1
1
IC50 = 1088 nM
   TI
   LI
   LO
   TS
CP0377322
3-{4-[1-(1,4-dioxa-spiro[4.5]dec-8-yl)-3-(4-trifluoromethoxy-phenyl)-ureidomethyl]-benzoylamino}-propionic acid
   Show/Hide
C27H30F3N3O7
 1
1
IC50 = 1207 nM
   TI
   LI
   LO
   TS
CP0377321
2-(4-((1-(4-tert-butylcyclohexyl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)benzamido)acetic acid
   Show/Hide
C28H34F3N3O5
 1
1
IC50 = 1700 nM
   TI
   LI
   LO
   TS
CP0502036
3-[[4-[[[1-(cyclopropanecarbonyl)piperidin-4-yl]-[[4-(trifluoromethoxy)phenyl]carbamoyl]amino]methyl]benzoyl]amino]propanoic acid
   Show/Hide
C28H31F3N4O6
 1
1
IC50 = 1984 nM
   TI
   LI
   LO
   TS
CP0502037
3-[[4-[[(4-tert-butylcyclohexyl)-[[4-(diethylcarbamoyl)phenyl]carbamoyl]amino]methyl]benzoyl]amino]propanoic acid
   Show/Hide
C33H46N4O5
 1
1
IC50 = 2429 nM
   TI
   LI
   LO
   TS
CP0559887
2-{4-[(3-Chloro-4-hydroxy-benzoyl)-hydrazonomethyl]-indol-1-yl}-N,N-diethyl-acetamide
   Show/Hide
C22H23ClN4O3
 1
1
IC50 = 2540 nM
   TI
   LI
   LO
   TS
CP0518065
1-(4-((2-(hydroxyamino)-2-oxoethyl)carbamoyl)benzyl)-1-(4-tert-butylcyclohexyl)-3-(4-(trifluoromethoxy)phenyl)urea
   Show/Hide
C28H35F3N4O5
 1
1
IC50 = 2960 nM
   TI
   LI
   LO
   TS
CP0254262
3-(4-((2-chloro-N-(3,3-diphenylpropyl)nicotinamido)methyl)benzamido)propanoic acid
   Show/Hide
C32H30ClN3O4
 1
1
IC50 = 7000 nM
   TI
   LI
   LO
   TS
CP0428128
1-(4-((3-amino-3-oxopropyl)carbamoyl)benzyl)-1-(4-tert-butylcyclohexyl)-3-(4-(trifluoromethoxy)phenyl)urea
   Show/Hide
C29H37F3N4O4
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0436885
4-(1-(4-((2-carboxyethyl)carbamoyl)benzyl)-3-(4-(trifluoromethoxy)phenyl)ureido)cyclohexanecarboxylic acid
   Show/Hide
C26H28F3N3O7
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0459753
4-(4-((1-(4-tert-butylcyclohexyl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)benzamido)butanoic acid
   Show/Hide
C30H38F3N3O5
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0459754
1-(4-((3-methoxypropyl)carbamoyl)benzyl)-1-(4-tert-butylcyclohexyl)-3-(4-(trifluoromethoxy)phenyl)urea
   Show/Hide
C30H40F3N3O4
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0526963
3-(4-((1-(4-((cyclopropylmethyl)carbamoyl)cyclohexyl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)benzamido)propanoic acid
   Show/Hide
C30H35F3N4O6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0536726
3-(4-((1-(4-(methylcarbamoyl)cyclohexyl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)benzamido)propanoic acid
   Show/Hide
C27H31F3N4O6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0538462
3-(4-((1-(4-methoxycyclohexyl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)benzamido)propanoic acid
   Show/Hide
C26H30F3N3O6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0553735
3-(4-((1-(4-tert-butylcyclohexyl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)benzamido)-3-methylbutanoic acid
   Show/Hide
C31H40F3N3O5
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0521152
2-(5-tert-Butyl-1H-benzoimidazol-2-ylsulfanyl)-1-(3,4-dihydroxy-phenyl)-ethanone
   Show/Hide
C19H20N2O3S
 1
1
Ki = 5400 nM
   TI
   LI
   LO
   TS
CP0454700
3-{2-[2-(3-Chloro-4-hydroxy-phenyl)-2-oxo-ethylsulfanyl]-1H-benzoimidazol-5-yloxymethyl}-benzoic acid methyl ester
   Show/Hide
C24H19ClN2O5S
 1
1
Ki = 9200 nM
   TI
   LI
   LO
   TS
CP0429195
2-(1H-Benzoimidazol-2-ylsulfanyl)-1-(3-chloro-4-hydroxy-phenyl)-ethanone
   Show/Hide
C15H11ClN2O2S
 1
1
Ki = 12000 nM
   TI
   LI
   LO
   TS
CP0514146
3-{2-[2-(3,4-Dihydroxy-phenyl)-2-oxo-ethylsulfanyl]-1H-benzoimidazol-5-yloxymethyl}-benzoic acid methyl ester
   Show/Hide
C24H20N2O6S
 1
1
Ki = 16000 nM
   TI
   LI
   LO
   TS
CP0461879
2-(5-Benzyloxy-1H-benzoimidazol-2-ylsulfanyl)-1-(3,4-dihydroxy-phenyl)-ethanone
   Show/Hide
C22H18N2O4S
 1
1
Ki = 18000 nM
   TI
   LI
   LO
   TS
CP0448583
2-(5,6-Dichloro-1H-benzoimidazol-2-ylsulfanyl)-1-(3,4-dihydroxy-phenyl)-ethanone
   Show/Hide
C15H10Cl2N2O3S
 1
1
Ki = 20000 nM
   TI
   LI
   LO
   TS
CP0356960
2-(1H-Benzoimidazol-2-ylsulfanyl)-1-(3,4-dihydroxy-phenyl)-ethanone
   Show/Hide
C15H12N2O3S
 1
1
Ki = 20000 nM
   TI
   LI
   LO
   TS
CP0524124
2-(1H-Benzoimidazol-2-ylsulfanyl)-1-(4-hydroxy-3-methoxy-phenyl)-ethanone
   Show/Hide
C16H14N2O3S
 1
1
Ki = 41000 nM
   TI
   LI
   LO
   TS
CP0329730
1-(3,4-dihydroxyphenyl)-2-[(6-methoxy-1H-benzimidazol-2-yl)sulfanyl]ethanone
   Show/Hide
C16H14N2O4S
 1
1
Ki = 42000 nM
   TI
   LI
   LO
   TS
CP0044776
1-(3,4-Dihydroxy-phenyl)-2-(5-phenyl-4H-[1,2,4]triazol-3-ylsulfanyl)-ethanone
   Show/Hide
C16H13N3O3S
 1
1
Ki = 55000 nM
   TI
   LI
   LO
   TS
CP0483065
1-(3,4-Dihydroxy-phenyl)-2-(5-nitro-1H-benzoimidazol-2-ylsulfanyl)-ethanone
   Show/Hide
C15H11N3O5S
 1
1
Ki = 55000 nM
   TI
   LI
   LO
   TS
CP0392592
2-(1H-Benzoimidazol-2-ylsulfanyl)-1-(4-hydroxy-phenyl)-ethanone
   Show/Hide
C15H12N2O2S
 1
1
Ki > 60000 nM
   TI
   LI
   LO
   TS
CP0148841
2-(Benzothiazol-2-ylsulfanyl)-1-(3,4-dihydroxy-phenyl)-ethanone
   Show/Hide
C15H11NO3S2
 1
1
Ki = 73000 nM
   TI
   LI
   LO
   TS
CP0534850
3-{2-[2-(3,4-Dihydroxy-phenyl)-2-oxo-ethylsulfanyl]-1H-benzoimidazol-5-yloxymethyl}-benzoic acid
   Show/Hide
C23H18N2O6S
 1
1
Ki = 95000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0134277
3-Cyano-4-hydroxy-benzoic acid [1-(2,3,5,6-tetramethyl-benzyl)-1H-indol-4-ylmethylene]-hydrazide
   Show/Hide
C28H26N4O2
 1
1 IC50 = 2.3 nM
CP0036234
4-[2-(4-Chloro-phenyl)-5-(2-phenoxy-phenyl)-3H-imidazol-4-yl]-pyridine
   Show/Hide
C26H18ClN3O
 2
1 IC50 = 6.5 nM
2 IC50 = 290 nM
CP0036294
4-[2-(4-Chloro-phenyl)-5-(3-phenoxy-phenyl)-3H-imidazol-4-yl]-pyridine
   Show/Hide
C26H18ClN3O
 2
1 IC50 = 13 nM
2 IC50 = 150 nM
CP0215714
4-[2-(4-Chloro-phenyl)-5-(2,4-dipropoxy-phenyl)-3H-imidazol-4-yl]-pyridine
   Show/Hide
C26H26ClN3O2
 2
1 IC50 = 13 nM
2 IC50 = 120 nM
CP0045459
3-Cyano-4-hydroxy-benzoic acid [1-[4-(4-isopropyl-benzyloxy)-3,5-dimethoxy-phenyl]-meth-(E)-ylidene]-hydrazide
   Show/Hide
C27H27N3O5
 1
1 IC50 = 20 nM
CP0245745
4-[2-(4-Chloro-phenyl)-5-(4-phenoxy-phenyl)-3H-imidazol-4-yl]-pyridine
   Show/Hide
C26H18ClN3O
 2
1 IC50 = 27 nM
2 IC50 = 110 nM
CP0112393
4-[4-(4-Fluoro-phenyl)-5-pyridin-4-yl-1H-pyrrol-2-yl]-benzonitrile
   Show/Hide
C22H14FN3
 1
1 IC50 = 50 nM
CP0144083
4-[3-(4-Fluoro-phenyl)-5-(4-nitro-phenyl)-1H-pyrrol-2-yl]-pyridine
   Show/Hide
C21H14FN3O2
 1
1 IC50 = 50 nM
CP0358493
3-Chloro-4-hydroxy-benzoic acid [1-[4-(4-isopropyl-benzyloxy)-naphthalen-1-yl]-meth-(E)-ylidene]-hydrazide
   Show/Hide
C28H25ClN2O3
 1
1 IC50 = 53 nM
CP0324497
4-[5-Biphenyl-3-yl-2-(4-chloro-phenyl)-3H-imidazol-4-yl]-pyridine
   Show/Hide
C26H18ClN3
 2
1 IC50 = 61 nM
2 IC50 > 3000 nM
CP0222549
4-[3-(3-Bromo-phenyl)-5-(4-chloro-phenyl)-1H-pyrrol-2-yl]-pyridine
   Show/Hide
C21H14BrClN2
 1
1 IC50 = 80.17 nM
CP0269118
3-Chloro-4-hydroxy-benzoic acid [1-(4-isopropyl-benzyl)-1H-indol-4-ylmethylene]-hydrazide
   Show/Hide
C26H24ClN3O2
 1
1 IC50 = 84 nM
CP0050171
4-[4-(4-Fluoro-phenyl)-5-pyridin-4-yl-1H-pyrrol-2-yl]-benzoic acid
   Show/Hide
C22H15FN2O2
 1
1 IC50 = 90.16 nM
CP0223176
(R)-1-[4-(4-Fluoro-phenyl)-2,6-diisopropyl-5-propyl-pyridin-3-yl]-ethanol
   Show/Hide
C22H30FNO
 1
1 IC50 = 110 nM
CP0259487
4-[5-(4-Fluoro-phenyl)-2-(4-methylsulfanyl-phenyl)-1H-imidazol-4-yl]-pyridine
   Show/Hide
C21H16FN3S
 2
1 IC50 = 117.22 nM
2 IC50 = 490 nM
CP0056450
4-[2-(4-Chloro-phenyl)-5-(4-iodo-phenyl)-3H-imidazol-4-yl]-pyridine
   Show/Hide
C20H13ClIN3
 2
1 IC50 = 130 nM
2 IC50 = 750 nM
CP0362260
2-{4-[(3-Chloro-4-hydroxy-benzoyl)-hydrazonomethyl]-naphthalen-1-yloxy}-N,N-diethyl-acetamide
   Show/Hide
C24H24ClN3O4
 1
1 IC50 = 130 nM
CP0297388
4-[5-Biphenyl-4-yl-2-(4-chloro-phenyl)-3H-imidazol-4-yl]-pyridine
   Show/Hide
C26H18ClN3
 2
1 IC50 = 140 nM
2 IC50 = 3800 nM
CP0202930
4-[3,5-Bis-(4-chloro-phenyl)-1H-pyrrol-2-yl]-pyridine
   Show/Hide
C21H14Cl2N2
 1
1 IC50 = 160.32 nM
CP0271630
4-[3-(4-Fluoro-phenyl)-1H-pyrrol-2-yl]-pyridine
   Show/Hide
C15H11FN2
 1
1 IC50 = 160.32 nM
CP0182277
4-[5-Cyclohexyl-3-(4-fluoro-phenyl)-1H-pyrrol-2-yl]-pyridine
   Show/Hide
C21H21FN2
 1
1 IC50 = 180.3 nM
CP0139955
4-[2,5-Bis-(4-chloro-phenyl)-3H-imidazol-4-yl]-pyridine
   Show/Hide
C20H13Cl2N3
 2
1 IC50 = 190 nM
2 IC50 = 2200 nM
CP0155748
5-Fluoro-2-(3-hydroxymethyl-2,6-diisopropyl-5-pentyl-pyridin-4-yl)-phenol
   Show/Hide
C23H32FNO2
 1
1 IC50 = 190 nM
CP0202931
4-[4-(4-Fluoro-phenyl)-5-pyridin-4-yl-1H-pyrrol-2-yl]-phenylamine
   Show/Hide
C21H16FN3
 1
1 IC50 = 190.11 nM
CP0129520
3-Chloro-4-hydroxy-benzoic acid (4-hydroxy-naphthalen-1-ylmethylene)-hydrazide
   Show/Hide
C18H13ClN2O3
 1
1 IC50 = 200 nM
CP0051820
4-[5-(4-Chloro-phenyl)-3-phenyl-1H-pyrrol-2-yl]-pyridine
   Show/Hide
C21H15ClN2
 1
1 IC50 = 210.38 nM
CP0222550
4-[4-(4-Fluoro-phenyl)-5-pyridin-4-yl-1H-pyrrol-2-yl]-benzoic acid ethyl ester
   Show/Hide
C24H19FN2O2
 1
1 IC50 = 260.02 nM
CP0166177
4-[2-(4-Bromo-phenyl)-5-(4-fluoro-phenyl)-3H-imidazol-4-yl]-pyridine
   Show/Hide
C20H13BrFN3
 2
1 IC50 = 270 nM
2 IC50 = 2900 nM
CP0038573
4-[3-(4-Bromo-phenyl)-5-(4-chloro-phenyl)-1H-pyrrol-2-yl]-pyridine
   Show/Hide
C21H14BrClN2
 1
1 IC50 = 300.61 nM
CP0085243
4-[3-(4-Fluoro-phenyl)-5-methyl-1H-pyrrol-2-yl]-pyridine
   Show/Hide
C16H13FN2
 1
1 IC50 = 320.63 nM
CP0222552
4-[3,5-Bis-(4-fluoro-phenyl)-1H-pyrrol-2-yl]-pyridine
   Show/Hide
C21H14F2N2
 1
1 IC50 = 340.41 nM
CP0057065
4-[2-(4-Chloro-phenyl)-5-(4-fluoro-phenyl)-3H-imidazol-4-yl]-pyridine
   Show/Hide
C20H13ClFN3
 2
1 IC50 = 400 nM
2 IC50 = 3200 nM
CP0063255
4-[5-(2,4-Dichloro-phenyl)-3-(4-fluoro-phenyl)-1H-pyrrol-2-yl]-pyridine
   Show/Hide
C21H13Cl2FN2
 1
1 IC50 = 420.73 nM
CP0313977
4-[5-(3-Chloro-phenyl)-3-(4-fluoro-phenyl)-1H-pyrrol-2-yl]-pyridine
   Show/Hide
C21H14ClFN2
 1
1 IC50 = 420.73 nM
CP0357281
4-[5-(4-Chloro-phenyl)-3-(3-methoxy-phenyl)-1H-pyrrol-2-yl]-pyridine
   Show/Hide
C22H17ClN2O
 1
1 IC50 = 420.73 nM
CP0276117
4-[5-(4-Fluoro-phenyl)-2-(4-iodo-phenyl)-3H-imidazol-4-yl]-pyridine
   Show/Hide
C20H13FIN3
 1
1 IC50 = 510 nM
CP0088613
4-[5-(4-Fluoro-phenyl)-2-(4-isopropyl-phenyl)-3H-imidazol-4-yl]-pyridine
   Show/Hide
C23H20FN3
 1
1 IC50 = 700 nM
CP0213431
[4-(4-fluorophenyl)-5-pentyl-2,6-di(propan-2-yl)pyridin-3-yl]methanol
   Show/Hide
C23H32FNO
 1
1 IC50 = 700 nM
CP0329193
4-[2-(4-Bromo-phenyl)-5-phenyl-3H-imidazol-4-yl]-pyridine
   Show/Hide
C20H14BrN3
 1
1 IC50 = 782 nM
CP0337062
4-[3-(4-Fluoro-phenyl)-5-phenyl-1H-pyrrol-2-yl]-pyridine
   Show/Hide
C21H15FN2
 1
1 IC50 = 801.68 nM
CP0287590
4-[3-(2-Bromo-phenyl)-5-(4-chloro-phenyl)-1H-pyrrol-2-yl]-pyridine
   Show/Hide
C21H14BrClN2
 1
1 IC50 = 1000 nM
CP0286734
4-[2-(4-Chloro-phenyl)-5-(4-fluoro-phenyl)-3H-imidazol-4-yl]-3-methyl-pyridine
   Show/Hide
C21H15ClFN3
 1
1 IC50 = 1100 nM
CP0310029
4-[5-(4-Chloro-phenyl)-3-(4-methoxy-phenyl)-1H-pyrrol-2-yl]-pyridine
   Show/Hide
C22H17ClN2O
 1
1 IC50 = 1150.8 nM
CP0324127
4-[5-(4-Fluoro-phenyl)-2-p-tolyl-3H-imidazol-4-yl]-pyridine
   Show/Hide
C21H16FN3
 1
1 IC50 = 1300 nM
CP0101935
4-[5-(4-Ethyl-phenyl)-3-(4-fluoro-phenyl)-1H-pyrrol-2-yl]-pyridine
   Show/Hide
C23H19FN2
 1
1 IC50 = 1361.44 nM
CP0303465
4-[2-(3-Bromo-phenyl)-5-(4-fluoro-phenyl)-3H-imidazol-4-yl]-pyridine
   Show/Hide
C20H13BrFN3
 1
1 IC50 = 1400 nM
CP0050873
(2,6-Diisopropyl-5-pentyl-4-phenyl-pyridin-3-yl)-methanol
   Show/Hide
C23H33NO
 1
1 IC50 = 1400 nM
CP0096778
4-[5-(4-Chloro-phenyl)-3-(4-fluoro-phenyl)-1H-pyrrol-2-yl]-pyridine
   Show/Hide
C21H14ClFN2
 1
1 IC50 = 1402.81 nM
CP0039137
4-[3-(5-Bromo-2-propoxy-phenyl)-5-(4-chloro-phenyl)-1H-pyrrol-2-yl]-pyridine
   Show/Hide
C24H20BrClN2O
 1
1 IC50 = 1442.12 nM
CP0078098
4-[5-(4-Fluoro-phenyl)-2-naphthalen-1-yl-3H-imidazol-4-yl]-pyridine
   Show/Hide
C24H16FN3
 1
1 IC50 = 1500 nM
CP0222551
4-[3-(4-Fluoro-phenyl)-5-p-tolyl-1H-pyrrol-2-yl]-pyridine
   Show/Hide
C22H17FN2
 1
1 IC50 = 1690.44 nM
CP0082326
4-[2,5-Bis-(4-fluoro-phenyl)-3H-imidazol-4-yl]-pyridine
   Show/Hide
C20H13F2N3
 1
1 IC50 = 2000 nM
CP0170867
4-[4-(4-Fluoro-phenyl)-5-pyridin-4-yl-1H-imidazol-2-yl]-phenylamine
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C20H15FN4
 1
1 IC50 = 2000 nM
CP0095585
4-[2-(5-Bromo-thiophen-2-yl)-5-(4-fluoro-phenyl)-3H-imidazol-4-yl]-pyridine
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C18H11BrFN3S
 1
1 IC50 = 2200 nM
CP0115930
4-[5-(4-Chloro-phenyl)-3-(2-methoxy-phenyl)-1H-pyrrol-2-yl]-pyridine
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C22H17ClN2O
 1
1 IC50 = 2654.61 nM
CP0295139
4-[3-(4-Fluoro-phenyl)-5-(4-methoxy-phenyl)-1H-pyrrol-2-yl]-pyridine
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C22H17FN2O
 1
1 IC50 = 2805.43 nM
CP0222548
4-[5-(4-Chloro-phenyl)-3-(2-propoxy-phenyl)-1H-pyrrol-2-yl]-pyridine
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C24H21ClN2O
 1
1 IC50 = 2844.46 nM
CP0222546
4-[5-(4-Chloro-phenyl)-3-(2-isobutoxy-phenyl)-1H-pyrrol-2-yl]-pyridine
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C25H23ClN2O
 1
1 IC50 = 3767.04 nM
CP0222547
4-[3-(2-Allyloxy-phenyl)-5-(4-chloro-phenyl)-1H-pyrrol-2-yl]-pyridine
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C24H19ClN2O
 1
1 IC50 = 4742.42 nM
CP0049626
[4-(4-fluorophenyl)-5-(2-methylprop-1-enyl)-2,6-di(propan-2-yl)pyridin-3-yl]methanol
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C22H28FNO
 1
1 IC50 = 7000 nM
CP0328303
4-[4-(4-Fluoro-phenyl)-5-pyridin-4-yl-1H-imidazol-2-yl]-benzonitrile
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C21H13FN4
 1
1 IC50 = 8000 nM
CP0345817
4-[4-(4-Fluoro-phenyl)-5-pyridin-4-yl-1H-imidazol-2-yl]-benzoic acid methyl ester
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C22H16FN3O2
 1
1 IC50 = 8700 nM
CP0217515
4-[2-Biphenyl-4-yl-5-(4-fluoro-phenyl)-3H-imidazol-4-yl]-pyridine
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C26H18FN3
 1
1 IC50 = 10000 nM
CP0139965
4-[5-(4-Fluoro-phenyl)-2-(4-methoxy-phenyl)-3H-imidazol-4-yl]-pyridine
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C21H16FN3O
 1
1 IC50 = 13000 nM
CP0280722
4-[5-(4-Chloro-phenyl)-3-(2-ethoxy-phenyl)-1H-pyrrol-2-yl]-pyridine
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C23H19ClN2O
 1
1 IC50 = 14223.29 nM
CP0057386
4-[5-(4-Fluoro-phenyl)-2-phenyl-3H-imidazol-4-yl]-pyridine
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C20H14FN3
 1
1 IC50 > 20000 nM
CP0406422
US8748624, 43
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C31H24ClF6N3O3
 1
1 Ki = 17.2 nM
CP0047783
3-{4-[1-(4-tert-Butyl-cyclohexyl)-3-(4-trifluoromethoxy-phenyl)-ureidomethyl]-benzoylamino}-propionic acid
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C29H36F3N3O5
 1
1 Ki = 63 nM
CP0120350
3-[[4-[(1S)-1-[3-(3,5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)pyrazol-1-yl]ethyl]benzoyl]amino]propanoic acid
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C32H27Cl2N3O4
 1
1 Ki = 70 nM
CP0070503
(R)-3-{4-[1-(4-Cyclohex-1-enylphenyl)-3-(3,5-dichlorophenyl)ureidomethyl]benzoylamino}-2-hydroxypropionic acid
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C30H29Cl2N3O5
 1
1 Ki = 85 nM
Clinical Information about the Protein
Target 1 ( Glucagon receptor (GCGR) )
Target Type Successful Target
Disease 3 Target-related Diseases  3
1 Hypoglycemia [ICD-11: 5A41]
2 Type-2 diabetes [ICD-11: 5A11]
3 Diabetic complication [ICD-11: 5A2Y]
Approved Drug(s) 1 Approved Drug  1
1 Glucagon recombinant Approved
Hypoglycemia
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 PF-06291874 Phase 2
Type-2 diabetes
Discontinued Drug(s) 1 Discontinued Drug  1
1 BAY-27-9955 Discontinued in Phase 1
Type-2 diabetes
Investigative Drug(s) 1 Investigative Drug  1
1 L-168049 Investigative
Diabetic complication
Target 2 ( Glucagon receptor messenger RNA (GCGR mRNA) )
Target Type Clinical trial Target
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT00676 Glucagon receptor Macaca mulatta, Rhesus macaque