General Information of the Protein
Protein ID
PT01231
Protein Name
MAP kinase-activated protein kinase 2
Gene Name
MAPKAPK2
Sequence
MLSNSQGQSPPVPFPAPAPPPQPPTPALPHPPAQPPPPPPQQFPQFHVKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSHNSLTTPCYTPYYVAPEVLGPEKYDKSCDMWSLGVIMYILLCGYPPFYSNHGLAISPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLKEDKERWEDVKEEMTSALATMRVDYEQIKIKKIEDASNPLLLKRRKKARALEAAALAH
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
CAMK protein kinase group
>
CAMK protein kinase MAPKAPK family
>
CAMK protein kinase MAPKAPK subfamily
Function
Stress-activated serine/threonine-protein kinase involved in cytokine production, endocytosis, reorganization of the cytoskeleton, cell migration, cell cycle control, chromatin remodeling, DNA damage response and transcriptional regulation. Following stress, it is phosphorylated and activated by MAP kinase p38-alpha/MAPK14, leading to phosphorylation of substrates. Phosphorylates serine in the peptide sequence, Hyd-X-R-X(2)-S, where Hyd is a large hydrophobic residue. Phosphorylates ALOX5, CDC25B, CDC25C, CEP131, ELAVL1, HNRNPA0, HSP27/HSPB1, KRT18, KRT20, LIMK1, LSP1, PABPC1, PARN, PDE4A, RCSD1, RPS6KA3, TAB3 and TTP/ZFP36. Phosphorylates HSF1; leading to the interaction with HSP90 proteins and inhibiting HSF1 homotrimerization, DNA-binding and transactivation activities (PubMed:16278218). Mediates phosphorylation of HSP27/HSPB1 in response to stress, leading to the dissociation of HSP27/HSPB1 from large small heat-shock protein (sHsps) oligomers and impairment of their chaperone activities and ability to protect against oxidative stress effectively. Involved in inflammatory response by regulating tumor necrosis factor (TNF) and IL6 production post-transcriptionally: acts by phosphorylating AU-rich elements (AREs)-binding proteins ELAVL1, HNRNPA0, PABPC1 and TTP/ZFP36, leading to the regulation of the stability and translation of TNF and IL6 mRNAs. Phosphorylation of TTP/ZFP36, a major post-transcriptional regulator of TNF, promotes its binding to 14-3-3 proteins and reduces its ARE mRNA affinity, leading to inhibition of dependent degradation of ARE-containing transcripts. Phosphorylates CEP131 in response to cellular stress induced by ultraviolet irradiation which promotes binding of CEP131 to 14-3-3 proteins and inhibits formation of novel centriolar satellites (PubMed:26616734). Also involved in late G2/M checkpoint following DNA damage through a process of post-transcriptional mRNA stabilization: following DNA damage, relocalizes from nucleus to cytoplasm and phosphorylates HNRNPA0 and PARN, leading to stabilization of GADD45A mRNA. Involved in toll-like receptor signaling pathway (TLR) in dendritic cells: required for acute TLR-induced macropinocytosis by phosphorylating and activating RPS6KA3.
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Uniprot ID
Primary ID:
P49137

Secondarily ID:
Q5SY30
Q5SY41
Q8IYD6
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Ensembl ID
ENSG00000162889
HGNC ID
HGNC:6887
Subcellular Location
Cytoplasm
Nucleus
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: CL000229 , SW1353
Compound ID Compound Name Compound Formula
CP0066026
5-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)-N-(pyridin-2-ylmethyl)furan-2-carboxamide
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C27H25ClN4O2
 1
1
EC50 = 350 nM
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CP0433457
5-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)-N-(pyridin-4-ylmethyl)furan-2-carboxamide
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C27H25ClN4O2
 1
1
EC50 = 530 nM
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CP0261806
5-(4-chlorophenyl)-N-ethyl-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C23H24ClN3O2
 1
1
EC50 = 800 nM
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CP0360905
2-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)-1,3-thiazole-4-carboxamide
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C20H19ClN4OS
 1
1
EC50 = 900 nM
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CP0333166
5-(4-chlorophenyl)-N-[4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl]furan-2-carboxamide
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C22H19ClN2O2
 1
1
EC50 = 1300 nM
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CP0156227
5-(4-chloro-2-methylphenyl)-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C22H22ClN3O2
 1
1
EC50 = 1400 nM
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CP0327714
5-(2,4-dichlorophenyl)-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C21H19Cl2N3O2
 1
1
EC50 = 1600 nM
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CP0262297
N-butyl-5-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C25H28ClN3O2
 1
1
EC50 = 1800 nM
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CP0536680
5-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)-1,2-oxazole-3-carboxamide
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C20H19ClN4O2
 1
1
EC50 = 1900 nM
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CP0066029
5-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C21H20ClN3O2
 1
1
EC50 = 2000 nM
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CP0337549
5-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)-N-propan-2-ylfuran-2-carboxamide
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C24H26ClN3O2
 1
1
EC50 = 2700 nM
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CP0156236
5-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)-N-propylfuran-2-carboxamide
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C24H26ClN3O2
 1
1
EC50 = 3000 nM
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CP0548177
6-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)pyridine-2-carboxamide
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C22H21ClN4O
 1
1
EC50 = 3900 nM
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CP0111166
5-(4-chlorophenyl)-N-[(1-methylimidazol-2-yl)methyl]-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C26H26ClN5O2
 1
1
EC50 = 4000 nM
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CP0536679
5-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)thiophene-2-carboxamide
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C21H20ClN3OS
 1
1
EC50 = 5000 nM
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CP0111164
5-(4-methoxyphenyl)-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C22H23N3O3
 1
1
EC50 = 8000 nM
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CP0111165
5-(4-chlorophenyl)-N-methyl-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C22H22ClN3O2
 1
1
EC50 = 9000 nM
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CP0327715
5-(4-chlorophenyl)-N-[4-(4-methyl-1-piperazinyl)phenyl]-2-furancarboxamide
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C22H22ClN3O2
 1
1
EC50 = 20000 nM
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CP0156229
5-(4-chlorophenyl)-N-(3-fluoro-4-piperazin-1-ylphenyl)furan-2-carboxamide
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C21H19ClFN3O2
 1
1
EC50 > 3400 nM
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CP0417358
5-(3-chlorophenyl)-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C21H20ClN3O2
 1
1
EC50 > 5000 nM
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CP0360904
N-(4-piperazin-1-ylphenyl)-5-[4-(trifluoromethyl)phenyl]furan-2-carboxamide
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C22H20F3N3O2
 1
1
EC50 > 7700 nM
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CP0066023
5-(5-chlorothiophen-2-yl)-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C19H18ClN3O2S
 1
1
EC50 > 8000 nM
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CP0066024
5-(4-chlorophenyl)-N-[4-piperazin-1-yl-2-(trifluoromethyl)phenyl]furan-2-carboxamide
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C22H19ClF3N3O2
 1
1
EC50 > 8000 nM
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CP0360901
5-(2-chlorophenyl)-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C21H20ClN3O2
 1
1
EC50 > 8000 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0211219
N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,3'-pyrrolidine]-2-yl)pyridin-2-yl]naphthalene-2-carboxamide
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C26H23N5O2
 1
1 EC50 = 0.62 nM
CP0095398
3,4-dimethyl-N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,3'-pyrrolidine]-2-yl)pyridin-2-yl]benzamide
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C24H25N5O2
 1
1 EC50 = 0.71 nM
CP0268229
N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,4'-piperidine]-2-yl)pyridin-2-yl]naphthalene-2-carboxamide
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C27H25N5O2
 1
1 EC50 = 0.72 nM
CP0354792
N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,4'-piperidine]-2-yl)pyridin-2-yl]naphthalene-1-carboxamide
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C27H25N5O2
 1
1 EC50 = 0.96 nM
CP0332147
3,4-dimethyl-N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,4'-piperidine]-2-yl)pyridin-2-yl]benzamide
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C25H27N5O2
 1
1 EC50 = 1 nM
CP0217029
3-fluoro-N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,4'-piperidine]-2-yl)pyridin-2-yl]benzamide
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C23H22FN5O2
 1
1 EC50 = 1.1 nM
CP0275367
4-fluoro-N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,3'-pyrrolidine]-2-yl)pyridin-2-yl]benzamide
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C22H20FN5O2
 1
1 EC50 = 1.3 nM
CP0222010
N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,4'-piperidine]-2-yl)pyridin-2-yl]pyridine-2-carboxamide
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C22H22N6O2
 1
1 EC50 = 1.4 nM
CP0222011
N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,4'-piperidine]-2-yl)pyridin-2-yl]-3-(trifluoromethoxy)benzamide
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C24H22F3N5O3
 1
1 EC50 = 1.5 nM
CP0268227
N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,4'-piperidine]-2-yl)pyridin-2-yl]-4-(trifluoromethyl)benzamide
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C24H22F3N5O2
 1
1 EC50 = 1.6 nM
CP0335269
N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,3'-pyrrolidine]-2-yl)pyridin-2-yl]-3-(trifluoromethoxy)benzamide
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C23H20F3N5O3
 1
1 EC50 = 1.6 nM
CP0337906
4-fluoro-N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,4'-piperidine]-2-yl)pyridin-2-yl]benzamide
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C23H22FN5O2
 1
1 EC50 = 1.6 nM
CP0268222
3-fluoro-N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,3'-pyrrolidine]-2-yl)pyridin-2-yl]benzamide
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C22H20FN5O2
 1
1 EC50 = 1.9 nM
CP0080969
3,4-dimethyl-N-[4-(1'-methyl-4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,4'-piperidine]-2-yl)pyridin-2-yl]benzamide
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C26H29N5O2
 1
1 EC50 = 2.3 nM
CP0095399
3,5-difluoro-N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,3'-piperidine]-2-yl)pyridin-2-yl]benzamide
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C23H21F2N5O2
 1
1 EC50 = 2.5 nM
CP0146233
3-fluoro-N-[4-(1'-methyl-4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,4'-piperidine]-2-yl)pyridin-2-yl]benzamide
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C24H24FN5O2
 1
1 EC50 = 2.5 nM
CP0211220
N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,4'-piperidine]-2-yl)pyridin-2-yl]pyridine-4-carboxamide
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C22H22N6O2
 1
1 EC50 = 2.6 nM
CP0282679
N-[4-(1'-methyl-4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,4'-piperidine]-2-yl)pyridin-2-yl]naphthalene-2-carboxamide
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C28H27N5O2
 1
1 EC50 = 2.6 nM
CP0146232
N-[4-(1'-methyl-4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,4'-piperidine]-2-yl)pyridin-2-yl]-3-(trifluoromethoxy)benzamide
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C25H24F3N5O3
 1
1 EC50 = 2.7 nM
CP0155454
N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,3'-piperidine]-2-yl)pyridin-2-yl]-3-(trifluoromethyl)benzamide
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C24H22F3N5O2
 1
1 EC50 = 3.3 nM
CP0136237
2'-(2-(benzo[d][1,3]dioxol-5-yl)pyrimidin-4-yl)-5',6'-dihydrospiro[piperidine-4,7'-pyrrolo[3,2-c]pyridin]-4'(1'H)-one
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C22H21N5O3
 2
1 EC50 = 4 nM
2 EC50 = 4.3 nM
CP0222008
N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,3'-pyrrolidine]-2-yl)pyridin-2-yl]pyridine-2-carboxamide
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C21H20N6O2
 1
1 EC50 = 4.1 nM
CP0275368
N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,3'-piperidine]-2-yl)pyridin-2-yl]pyridine-2-carboxamide
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C22H22N6O2
 1
1 EC50 = 4.2 nM
CP0085235
N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,3'-piperidine]-2-yl)pyridin-2-yl]naphthalene-1-carboxamide
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C27H25N5O2
 1
1 EC50 = 5.1 nM
CP0136273
2'-(2-(benzofuran-2-yl)pyrimidin-4-yl)-5',6'-dihydrospiro[piperidine-4,7'-pyrrolo[3,2-c]pyridin]-4'(1'H)-one
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C23H21N5O2
 1
1 EC50 = 5.9 nM
CP0035328
(S)-2'-(2-(pyridin-3-yl)pyrimidin-4-yl)-5',6'-dihydrospiro[piperidine-3,7'-pyrrolo[3,2-c]pyridin]-4'(1'H)-one
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C20H20N6O
 1
1 EC50 = 6.5 nM
CP0035338
(S)-2'-(2-(6-(3-methoxypropoxy)pyridin-3-yl)pyrimidin-4-yl)-5',6'-dihydrospiro[piperidine-3,7'-pyrrolo[3,2-c]pyridin]-4'(1'H)-one
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C24H28N6O3
 1
1 EC50 = 6.9 nM
CP0136275
(S)-2'-(2-(benzo[d][1,3]dioxol-5-yl)pyrimidin-4-yl)-5',6'-dihydrospiro[piperidine-3,7'-pyrrolo[3,2-c]pyridin]-4'(1'H)-one
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C22H21N5O3
 1
1 EC50 = 7.4 nM
CP0335270
N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,3'-piperidine]-2-yl)pyridin-2-yl]-4-(trifluoromethyl)benzamide
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C24H22F3N5O2
 1
1 EC50 = 9.1 nM
CP0250562
(S)-2'-(2-(5-methoxypyridin-3-yl)pyrimidin-4-yl)-5',6'-dihydrospiro[piperidine-3,7'-pyrrolo[3,2-c]pyridin]-4'(1'H)-one
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C21H22N6O2
 1
1 EC50 = 9.3 nM
CP0209410
N-[4-(4-oxospiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,3'-piperidine]-2-yl)pyridin-2-yl]-3-(trifluoromethoxy)benzamide
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C24H22F3N5O3
 1
1 EC50 = 11 nM
CP0035346
2'-(2-(benzofuran-2-yl)pyrimidin-4-yl)-1-methyl-5',6'-dihydrospiro[piperidine-4,7'-pyrrolo[3,2-c]pyridin]-4'(1'H)-one
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C24H23N5O2
 1
1 EC50 = 13 nM
CP0035349
2-(2-pyridin-3-ylpyrimidin-4-yl)spiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,3'-piperidine]-4-one
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C20H20N6O
 1
1 EC50 = 18 nM
CP0035326
2-[2-[6-(3-methoxypropoxy)pyridin-3-yl]pyrimidin-4-yl]spiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,3'-piperidine]-4-one
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C24H28N6O3
 1
1 EC50 = 21 nM
CP0035348
2-[2-(5-methoxypyridin-3-yl)pyrimidin-4-yl]spiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,3'-piperidine]-4-one
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C21H22N6O2
 1
1 EC50 = 24 nM
CP0035344
2-[2-(1,3-benzodioxol-5-yl)pyrimidin-4-yl]spiro[5,6-dihydro-1H-pyrrolo[3,2-c]pyridine-7,3'-piperidine]-4-one
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C22H21N5O3
 1
1 EC50 = 28 nM
CP0035340
2'-(2-(benzofuran-2-yl)pyrimidin-4-yl)-1-ethyl-5',6'-dihydrospiro[piperidine-4,7'-pyrrolo[3,2-c]pyridin]-4'(1'H)-one
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C25H25N5O2
 1
1 EC50 = 59 nM
CP0170204
(R)-2'-(2-(benzo[d][1,3]dioxol-5-yl)pyrimidin-4-yl)-5',6'-dihydrospiro[piperidine-3,7'-pyrrolo[3,2-c]pyridin]-4'(1'H)-one
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C22H21N5O3
 1
1 EC50 = 91 nM
CP0241914
(R)-2'-(2-(5-methoxypyridin-3-yl)pyrimidin-4-yl)-5',6'-dihydrospiro[piperidine-3,7'-pyrrolo[3,2-c]pyridin]-4'(1'H)-one
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C21H22N6O2
 1
1 EC50 = 126 nM
CP0250569
(R)-2'-(2-(6-(3-methoxypropoxy)pyridin-3-yl)pyrimidin-4-yl)-5',6'-dihydrospiro[piperidine-3,7'-pyrrolo[3,2-c]pyridin]-4'(1'H)-one
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C24H28N6O3
 1
1 EC50 = 129 nM
CP0035345
(R)-2'-(2-(pyridin-3-yl)pyrimidin-4-yl)-5',6'-dihydrospiro[piperidine-3,7'-pyrrolo[3,2-c]pyridin]-4'(1'H)-one
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C20H20N6O
 1
1 EC50 = 288 nM
CP0049116
Pyrrolopyridine, 23
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C18H14FN3O
 3
1 EC50 = 372 nM
2 IC50 = 126 nM
3 IC50 = 560 nM
CP0297493
(R)-10-Methyl-9,10,11,12-tetrahydro-7-thia-4,9,12-triaza-naphtho[1,2-a]azulen-8-one
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C15H13N3OS
 1
1 IC50 = 1 nM
CP0225618
4-[4-oxo-8-piperazin-1-yl-5-[(2-pyrimidin-5-ylphenyl)methyl]-10H-furo[2,3-c][1]benzazepin-2-yl]benzonitrile
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C34H28N6O2
 1
1 IC50 = 1.9 nM
CP0035410
N-[1-(2,2-dimethylpropyl)piperidin-4-yl]-2-[(1-oxospiro[2,3-dihydropyrazino[1,2-a]indole-4,1'-cyclobutane]-7-carbonyl)amino]-1,3-thiazole-4-carboxamide
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C29H36N6O3S
 1
1 IC50 = 2 nM
CP0137647
(R)-3-Chloro-10-methyl-9,10,11,12-tetrahydro-7-thia-4,9,12-triaza-naphtho[1,2-a]azulen-8-one
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C15H12ClN3OS
 1
1 IC50 = 2 nM
CP0186922
(15R)-15-methyl-5-(6-methylpyridin-3-yl)-11-thia-6,14,17-triazatetracyclo[8.8.0.02,7.012,18]octadeca-1(10),2(7),3,5,8,12(18)-hexaen-13-one
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C21H18N4OS
 3
1 IC50 = 2 nM
2 IC50 = 5 nM
3 Ki = 5 nM
CP0191246
4-(15-piperazin-1-yl-8-oxa-2,5-diazatetracyclo[11.4.0.02,6.07,11]heptadeca-1(13),3,5,7(11),9,14,16-heptaen-9-yl)benzonitrile
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C25H21N5O
 1
1 IC50 = 2.9 nM
CP0169211
4-(4-methoxyphenyl)-1'-methylspiro[3,5,13,17-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C23H23N5O2
 1
1 IC50 < 3 nM
CP0243150
4-[5-(3-methoxypropoxy)pyridin-3-yl]-1'-methylspiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C26H29N5O3
 1
1 IC50 < 3 nM
CP0243802
1'-ethyl-4-(2-fluorophenyl)spiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C24H23FN4O
 1
1 IC50 < 3 nM
CP0255889
4-(2-fluorophenyl)-1'-methylspiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C23H21FN4O
 1
1 IC50 < 3 nM
CP0262877
4-(3-fluorophenyl)-1'-methylspiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C23H21FN4O
 1
1 IC50 < 3 nM
CP0262878
1'-methyl-4-[4-(2-morpholin-4-ylethoxy)phenyl]spiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C29H33N5O3
 1
1 IC50 < 3 nM
CP0314162
1'-methyl-4-[4-(2-morpholin-4-ylethoxy)phenyl]spiro[3,5,13,17-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C28H32N6O3
 1
1 IC50 < 3 nM
CP0315123
4-(6-fluoropyridin-3-yl)-1'-methylspiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C22H20FN5O
 1
1 IC50 < 3 nM
CP0337966
4-(3-fluorophenyl)spiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C22H19FN4O
 1
1 IC50 < 3 nM
CP0337967
4-(4-methoxyphenyl)-1'-methylspiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C24H24N4O2
 1
1 IC50 < 3 nM
CP0197173
4-(15-piperazin-1-yl-8-oxa-2,4,5-triazatetracyclo[11.4.0.02,6.07,11]heptadeca-1(13),3,5,7(11),9,14,16-heptaen-9-yl)benzonitrile
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C24H20N6O
 1
1 IC50 = 3.8 nM
CP0262879
4-(2-fluorophenyl)-1'-methylspiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,4'-piperidine]-12-one
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C25H25FN4O
 1
1 IC50 = 4 nM
CP0127758
(R)-10-Methyl-3-(4-methyl-pyridin-3-yl)-9,10,11,12-tetrahydro-7-thia-4,9,12-triaza-naphtho[1,2-a]azulen-8-one
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C21H18N4OS
 1
1 IC50 = 5 nM
CP0152816
(R)-10-Methyl-3-pyridin-3-yl-9,10,11,12-tetrahydro-7-thia-4,9,12-triaza-naphtho[1,2-a]azulen-8-one
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C20H16N4OS
 1
1 IC50 = 5 nM
CP0274491
(3R)-3-(aminomethyl)-9-methoxy-1,2,3,4-tetrahydro-5H-[1]benzothieno[3,2-e][1,4]diazepin-5-one
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C13H15N3O2S
 1
1 IC50 = 5 nM
CP0170947
4-[5-(2-methoxyethoxy)pyridin-3-yl]-5,13,16-triazatetracyclo[8.6.0.02,7.011,15]hexadeca-1(10),2,4,6,8,11(15)-hexaen-12-one
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C21H18N4O3
 1
1 IC50 = 5 nM
CP0290793
4-[5-(2-morpholin-4-ylethoxy)pyridin-3-yl]-5,13,16-triazatetracyclo[8.6.0.02,7.011,15]hexadeca-1(10),2,4,6,8,11(15)-hexaen-12-one
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C24H23N5O3
 1
1 IC50 = 5 nM
CP0286936
4-(3-fluorophenyl)-1'-methylspiro[3,5,13,17-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C22H20FN5O
 1
1 IC50 = 6 nM
CP0291497
4-[5-(2-methoxyethoxy)pyridin-3-yl]-1'-methylspiro[3,5,13,17-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C24H26N6O3
 1
1 IC50 = 6 nM
CP0160608
4-(6-fluoropyridin-3-yl)-1'-methylspiro[3,5,13,17-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C21H19FN6O
 1
1 IC50 = 7 nM
CP0341838
9-(4-chlorophenyl)-15-piperazin-1-yl-8-oxa-2,5-diazatetracyclo[11.4.0.02,6.07,11]heptadeca-1(13),3,5,7(11),9,14,16-heptaene
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C24H21ClN4O
 1
1 IC50 = 7 nM
CP0243803
4-(3-fluorophenyl)-5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaen-12-one
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C20H16FN3O
 1
1 IC50 = 8 nM
CP0127755
(R)-10-Methyl-3-phenyl-9,10,11,12-tetrahydro-7-thia-4,9,12-triaza-naphtho[1,2-a]azulen-8-one
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C21H17N3OS
 1
1 IC50 = 9 nM
CP0079816
9-(4-chlorophenyl)-3-methyl-15-piperazin-1-yl-8-oxa-2,5-diazatetracyclo[11.4.0.02,6.07,11]heptadeca-1(13),3,5,7(11),9,14,16-heptaene
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C25H23ClN4O
 1
1 IC50 = 9.2 nM
CP0298453
9-(4-chlorophenyl)-15-piperazin-1-yl-8-oxa-2,4,5-triazatetracyclo[11.4.0.02,6.07,11]heptadeca-1(13),3,5,7(11),9,14,16-heptaene
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C23H20ClN5O
 1
1 IC50 = 9.3 nM
CP0073084
4-[5-(2-methoxyethoxy)pyridin-3-yl]-5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,8,11(16)-hexaen-12-one
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C22H20N4O3
 2
1 IC50 = 10 nM
2 IC50 = 12 nM
CP0271340
4-[5-(2-morpholin-4-ylethoxy)pyridin-3-yl]-5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,8,11(16)-hexaen-12-one
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C25H25N5O3
 1
1 IC50 = 10 nM
CP0299915
4-(4-methoxyphenyl)spiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-14,3'-azetidine]-12-one
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C23H22N4O2
 1
1 IC50 = 12 nM
CP0243804
4-(2-fluorophenyl)-1',17-dimethylspiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C24H23FN4O
 1
1 IC50 = 13 nM
CP0092483
(R)-10-Methyl-3-pyridin-4-yl-9,10,11,12-tetrahydro-7-thia-4,9,12-triaza-naphtho[1,2-a]azulen-8-one
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C20H16N4OS
 1
1 IC50 = 14 nM
CP0371189
(R)-3-(2-Fluoro-phenyl)-10-methyl-9,10,11,12-tetrahydro-7-thia-4,9,12-triaza-naphtho[1,2-a]azulen-8-one
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C21H16FN3OS
 1
1 IC50 = 14 nM
CP0167552
(S)-7-Hydroxymethyl-3-methoxy-5,6,7,8-tetrahydro-10-thia-5,8-diaza-benzo[a]azulen-9-one
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C13H14N2O3S
 1
1 IC50 = 14 nM
CP0315870
4-(3-fluoro-4-methoxyphenyl)-5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,8,11(16)-hexaen-12-one
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C21H16FN3O2
 1
1 IC50 = 15 nM
CP0358091
(R)-9-Methyl-8,9,10,11-tetrahydro-3-oxa-6-thia-8,11-diaza-cyclohepta[b]-as-indacen-7-one
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C14H12N2O2S
 1
1 IC50 = 16 nM
CP0303239
4-[3-(2-morpholin-4-ylethoxy)phenyl]-5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,8,11(16)-hexaen-12-one
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C26H26N4O3
 1
1 IC50 = 16 nM
CP0262880
4-(2-fluorophenyl)spiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C22H19FN4O
 1
1 IC50 = 17 nM
CP0298567
(R)-3-(2-Methoxy-phenyl)-10-methyl-9,10,11,12-tetrahydro-7-thia-4,9,12-triaza-naphtho[1,2-a]azulen-8-one
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C22H19N3O2S
 1
1 IC50 = 20 nM
CP0255892
4-(2-fluorophenyl)-17-methylspiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C23H21FN4O
 1
1 IC50 = 20 nM
CP0152814
(R)-10-Methyl-3-pyrimidin-5-yl-9,10,11,12-tetrahydro-7-thia-4,9,12-triaza-naphtho[1,2-a]azulen-8-one
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C19H15N5OS
 1
1 IC50 = 23 nM
CP0313128
4-(4-methoxyphenyl)-14-methyl-5,13,14,17-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,8,11(16)-hexaen-12-one
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C21H18N4O2
 1
1 IC50 = 23 nM
CP0090196
1-[4-[2-[5-(4-chlorophenyl)furan-2-yl]imidazol-1-yl]phenyl]piperazine
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C23H21ClN4O
 1
1 IC50 = 25.5 nM
CP0309046
4-(6-fluoropyridin-3-yl)spiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,1'-cyclopropane]-12-one
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C21H17FN4O
 1
1 IC50 = 27 nM
CP0136228
(R)-9-Methyl-1,2,8,9,10,11-hexahydro-3-oxa-6-thia-8,11-diaza-cyclohepta[b]-as-indacen-7-one
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C14H14N2O2S
 1
1 IC50 = 28 nM
CP0137650
(R)-10-Methyl-3-o-tolyl-9,10,11,12-tetrahydro-7-thia-4,9,12-triaza-naphtho[1,2-a]azulen-8-one
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C22H19N3OS
 1
1 IC50 = 30 nM
CP0298573
(R)-3-Isobutoxy-7-methyl-5,6,7,8-tetrahydro-10-thia-5,8-diaza-benzo[a]azulen-9-one
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C16H20N2O2S
 1
1 IC50 = 30 nM
CP0169838
3-[5-(4-chlorophenyl)furan-2-yl]-4-(4-piperazin-1-ylphenyl)-5-pyridin-2-yl-5H-1,2,4-oxadiazole
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C27H24ClN5O2
 1
1 IC50 = 30 nM
CP0550526
3-[5-(4-chlorophenyl)furan-2-yl]-4-(4-piperazin-1-ylphenyl)-5-pyridin-4-yl-5H-1,2,4-oxadiazole
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C27H24ClN5O2
 1
1 IC50 = 30 nM
CP0283485
4-[3-(2-morpholin-4-ylethoxy)phenyl]-5,13,16-triazatetracyclo[8.6.0.02,7.011,15]hexadeca-1(10),2,4,6,8,11(15)-hexaen-12-one
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C25H24N4O3
 1
1 IC50 = 32 nM
CP0262881
4-(2-fluorophenyl)-1'-methylspiro[3,5,13,17-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C22H20FN5O
 1
1 IC50 = 34 nM
CP0332074
4-(2-fluorophenyl)-5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaen-12-one
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C20H16FN3O
 1
1 IC50 = 37 nM
CP0273764
(R)-3-Methoxy-7-methyl-5,6,7,8-tetrahydro-10-thia-5,8-diaza-benzo[a]azulen-9-one
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C13H14N2O2S
 1
1 IC50 = 40 nM
CP0309047
4-[5-(2-methoxyethoxy)pyridin-3-yl]-5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaen-12-one
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C22H22N4O3
 1
1 IC50 = 40 nM
CP0133903
3-[5-(4-chlorophenyl)furan-2-yl]-4-(4-piperazin-1-ylphenyl)-5-(2-pyrimidin-5-ylphenyl)-5H-1,2,4-oxadiazole
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C32H27ClN6O2
 1
1 IC50 = 40 nM
CP0137649
(R)-3-(3-Methoxy-phenyl)-10-methyl-9,10,11,12-tetrahydro-7-thia-4,9,12-triaza-naphtho[1,2-a]azulen-8-one
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C22H19N3O2S
 1
1 IC50 = 41 nM
CP0310194
4-(4-methoxyphenyl)-1'-methylspiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-14,3'-azetidine]-12-one
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C24H24N4O2
 1
1 IC50 = 45 nM
CP0309048
4-(6-fluoropyridin-3-yl)spiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-14,1'-cyclopropane]-12-one
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C21H17FN4O
 1
1 IC50 = 50 nM
CP0169836
3-[5-(4-chlorophenyl)furan-2-yl]-5-phenyl-4-(4-piperazin-1-ylphenyl)-5H-1,2,4-oxadiazole
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C28H25ClN4O2
 1
1 IC50 = 50 nM
CP0340195
3-[5-(4-fluorophenyl)furan-2-yl]-4-(4-piperazin-1-ylphenyl)-5-(2-pyrimidin-5-ylphenyl)-5H-1,2,4-oxadiazole
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C32H27FN6O2
 1
1 IC50 = 50 nM
CP0085000
6-methyl-7-N-(2-methyl-1,3-benzothiazol-6-yl)-5-N-[(3S)-piperidin-3-yl]pyrazolo[1,5-a]pyrimidine-5,7-diamine
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C20H23N7S
 1
1 IC50 = 54 nM
CP0329348
3-[5-(4-chlorophenyl)furan-2-yl]-5-(5-fluoropyridin-2-yl)-4-(4-piperazin-1-ylphenyl)-5H-1,2,4-oxadiazole
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C27H23ClFN5O2
 1
1 IC50 = 60 nM
CP0338515
3-[5-(4-chlorophenyl)furan-2-yl]-5-(1H-imidazol-5-yl)-4-(4-piperazin-1-ylphenyl)-5H-1,2,4-oxadiazole
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C25H23ClN6O2
 1
1 IC50 = 70 nM
CP0046929
4-(4-methoxyphenyl)-5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaen-12-one
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C21H19N3O2
 1
1 IC50 = 80 nM
CP0297522
4-[5-(2-morpholin-4-ylethoxy)pyridin-3-yl]-5,13,18-triazatetracyclo[8.8.0.02,7.011,17]octadeca-1(10),2,4,6,8,11(17)-hexaen-12-one
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C26H27N5O3
 1
1 IC50 = 80 nM
CP0313129
4-(2-fluorophenyl)-5,13,16-triazatetracyclo[8.6.0.02,7.011,15]hexadeca-1(10),2,4,6,8,11(15)-hexaen-12-one
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C19H12FN3O
 1
1 IC50 = 85 nM
CP0433457
5-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)-N-(pyridin-4-ylmethyl)furan-2-carboxamide
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C27H25ClN4O2
 1
1 IC50 = 90 nM
CP0038368
4-[5-(2-methoxyethoxy)pyridin-3-yl]-5,13,18-triazatetracyclo[8.8.0.02,7.011,17]octadeca-1(10),2,4,6,8,11(17)-hexaen-12-one
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C23H22N4O3
 1
1 IC50 = 96 nM
CP0258055
4-(3-fluorophenyl)spiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,1'-cyclopropane]-12-one
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C22H18FN3O
 1
1 IC50 = 100 nM
CP0262882
4-[4-(2-morpholin-4-ylethoxy)phenyl]spiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-14,1'-cyclopropane]-12-one
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C28H30N4O3
 1
1 IC50 = 100 nM
CP0111166
5-(4-chlorophenyl)-N-[(1-methylimidazol-2-yl)methyl]-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C26H26ClN5O2
 1
1 IC50 = 100 nM
CP0338517
3-[5-(4-chlorophenyl)furan-2-yl]-4-(4-piperazin-1-ylphenyl)-5-(4-pyrimidin-5-ylphenyl)-5H-1,2,4-oxadiazole
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C32H27ClN6O2
 1
1 IC50 = 100 nM
CP0274493
(R)-3-(3-Methoxy-benzyloxy)-7-methyl-5,6,7,8-tetrahydro-10-thia-5,8-diaza-benzo[a]azulen-9-one
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C20H20N2O3S
 1
1 IC50 = 110 nM
CP0066026
5-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)-N-(pyridin-2-ylmethyl)furan-2-carboxamide
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C27H25ClN4O2
 1
1 IC50 = 110 nM
CP0302459
1'-acetyl-4-(2-fluorophenyl)spiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C24H21FN4O2
 1
1 IC50 = 120 nM
CP0310195
4-(6-fluoropyridin-3-yl)spiro[3,5,13,17-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-14,1'-cyclopropane]-12-one
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C20H16FN5O
 1
1 IC50 = 120 nM
CP0708510
1,3-Diamino-6,7-dihydroxy-9,9a-dihydro-4aH-xanthene-2-carbonitrile
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C14H11N3O3
 1
1 IC50 = 130 nM
CP0073086
4-(4-methoxyphenyl)spiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,1'-cyclopropane]-12-one
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C23H21N3O2
 1
1 IC50 = 130 nM
CP0261806
5-(4-chlorophenyl)-N-ethyl-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C23H24ClN3O2
 1
1 IC50 = 130 nM
CP0019579
7-N-(4-ethoxyphenyl)-6-methyl-5-N-[(3S)-piperidin-3-yl]pyrazolo[1,5-a]pyrimidine-5,7-diamine
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C20H26N6O
 2
1 IC50 = 130 nM
2 IC50 = 11000 nM
CP0257194
7-N-[4-(2-methoxyethoxy)phenyl]-6-methyl-5-N-[(3S)-piperidin-3-yl]pyrazolo[1,5-a]pyrimidine-5,7-diamine
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C21H28N6O2
 1
1 IC50 = 130 nM
CP0302460
4-(2-fluorophenyl)spiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-14,1'-cyclopropane]-12-one
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C22H18FN3O
 1
1 IC50 = 140 nM
CP0507894
(R)-9-Methyl-2-phenyl-8,9,10,11-tetrahydro-3-oxa-6-thia-8,11-diaza-cyclohepta[b]-as-indacen-7-one
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C20H16N2O2S
 1
1 IC50 = 150 nM
CP0332075
4-(4-methoxyphenyl)spiro[3,5,13,17-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,1'-cyclopropane]-12-one
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C22H20N4O2
 1
1 IC50 = 150 nM
CP0270953
4-(3-fluoro-4-methoxyphenyl)-5,16-diazatetracyclo[8.6.0.02,7.011,15]hexadeca-1(10),2,4,6,8,11(15)-hexaen-12-one
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C21H15FN2O2
 1
1 IC50 = 160 nM
CP0302461
4-(4-methoxyphenyl)spiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-14,1'-cyclopropane]-12-one
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C23H21N3O2
 1
1 IC50 = 175 nM
CP0843985
1,3-Diamino-6-hydroxy-9,9a-dihydro-4aH-xanthene-2-carbonitrile
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C14H11N3O2
 1
1 IC50 = 180 nM
CP0298570
3-Methoxy-5,6,7,8-tetrahydro-10-thia-5,8-diaza-benzo[a]azulen-9-one
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C12H12N2O2S
 1
1 IC50 = 180 nM
CP0048734
4-[4-(2-morpholin-4-ylethoxy)phenyl]spiro[3,5,13,17-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-14,1'-cyclopropane]-12-one
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C27H29N5O3
 1
1 IC50 = 180 nM
CP0086560
4-[5-(2-methoxyethoxy)pyridin-3-yl]-5,14,18-triazatetracyclo[9.7.0.02,7.012,17]octadeca-1(11),2,4,6,12(17)-pentaen-13-one
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C23H24N4O3
 1
1 IC50 = 180 nM
CP0299507
(R)-3-Hydroxy-7-methyl-5,6,7,8-tetrahydro-10-thia-5,8-diaza-benzo[a]azulen-9-one
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C12H12N2O2S
 1
1 IC50 = 190 nM
CP0299918
4-(3-fluorophenyl)spiro[17-oxa-5,13-diazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C22H18FN3O2
 1
1 IC50 = 200 nM
CP0046930
12-(2-fluorophenyl)-1'-methylspiro[4,8,13-triazatetracyclo[7.7.0.02,7.010,15]hexadeca-1(9),2(7),10,12,14-pentaene-6,3'-azetidine]-3-one
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C22H19FN4O
 1
1 IC50 = 230 nM
CP0243805
4-(3-fluorophenyl)spiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-14,1'-cyclopropane]-12-one
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C22H18FN3O
 1
1 IC50 = 230 nM
CP0314163
1'-(2-fluoroethyl)-4-(2-fluorophenyl)spiro[5,13,17-triazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-15,3'-azetidine]-12-one
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C24H22F2N4O
 1
1 IC50 = 230 nM
CP0137687
(R)-3-(2-Methoxy-ethoxy)-7-methyl-5,6,7,8-tetrahydro-10-thia-5,8-diaza-benzo[a]azulen-9-one
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C15H18N2O3S
 1
1 IC50 = 270 nM
CP0255897
4-(4-methoxyphenyl)-3,5,13,17-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaen-12-one
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C20H18N4O2
 1
1 IC50 = 270 nM
CP0092575
(S)-3-Methoxy-7-methyl-5,6,7,8-tetrahydro-10-thia-5,8-diaza-benzo[a]azulen-9-one
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C13H14N2O2S
 1
1 IC50 = 300 nM
CP0766369
1,3-Diamino-6,7-dimethoxy-9,9a-dihydro-4aH-xanthene-2-carbonitrile
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C16H15N3O3
 1
1 IC50 = 330 nM
CP0262297
N-butyl-5-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C25H28ClN3O2
 1
1 IC50 = 440 nM
CP0298994
(R)-3-Methoxy-7-propylaminomethyl-5,6,7,8-tetrahydro-10-thia-5,8-diaza-benzo[a]azulen-9-one
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C16H21N3O2S
 1
1 IC50 = 450 nM
CP0774060
1,3-Diamino-5-hydroxy-9,9a-dihydro-4aH-xanthene-2-carbonitrile
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C14H11N3O2
 1
1 IC50 = 460 nM
CP0778265
1,3-Diamino-7-hydroxy-9,9a-dihydro-4aH-xanthene-2-carbonitrile
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C14H11N3O2
 1
1 IC50 = 470 nM
CP0778266
8,10-Diamino-2,3,10a,11-tetrahydro-6aH-1,4,6-trioxa-naphthacene-9-carbonitrile
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C16H13N3O3
 1
1 IC50 = 490 nM
CP0299506
3-Methoxy-5,6,7,8-tetrahydro-10-thia-8-aza-benzo[a]azulen-9-one
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C13H13NO2S
 1
1 IC50 = 500 nM
CP0776397
1,3,7-Triamino-9,9a-dihydro-4aH-xanthene-2-carbonitrile
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C14H12N4O
 1
1 IC50 = 530 nM
CP0843986
1,3-Diamino-9,9a-dihydro-4aH-xanthene-2-carbonitrile
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C14H11N3O
 1
1 IC50 = 560 nM
CP0297496
(R)-7-Ethylaminomethyl-3-methoxy-5,6,7,8-tetrahydro-10-thia-5,8-diaza-benzo[a]azulen-9-one
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C15H19N3O2S
 1
1 IC50 = 570 nM
CP0302327
(R)-7-(Benzylamino-methyl)-3-methoxy-5,6,7,8-tetrahydro-10-thia-5,8-diaza-benzo[a]azulen-9-one
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C20H21N3O2S
 1
1 IC50 = 570 nM
CP0111165
5-(4-chlorophenyl)-N-methyl-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C22H22ClN3O2
 1
1 IC50 = 600 nM
CP0806762
1,3-Diamino-6-[1,4]dioxan-2-yl-7-hydroxy-9,9a-dihydro-4aH-xanthene-2-carbonitrile
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C18H17N3O4
 1
1 IC50 = 620 nM
CP0156236
5-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)-N-propylfuran-2-carboxamide
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C24H26ClN3O2
 1
1 IC50 = 650 nM
CP0773756
1,3-Diamino-6,8-dihydroxy-9,9a-dihydro-4aH-xanthene-2-carbonitrile
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C14H11N3O3
 1
1 IC50 = 690 nM
CP0711470
1,3-Diamino-6-ethoxy-7-hydroxy-9,9a-dihydro-4aH-xanthene-2-carbonitrile
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C16H15N3O3
 1
1 IC50 = 770 nM
CP0777931
1,3-Diamino-5,6-dihydroxy-9,9a-dihydro-4aH-xanthene-2-carbonitrile
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C14H11N3O3
 1
1 IC50 = 850 nM
CP0347053
4-(2-fluorophenyl)spiro[3,5,13,17-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-14,1'-cyclopropane]-12-one
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C21H17FN4O
 1
1 IC50 = 860 nM
CP0074188
4-(4-methoxyphenyl)spiro[3,5,13,17-tetrazatetracyclo[8.7.0.02,7.011,16]heptadeca-1(10),2,4,6,11(16)-pentaene-14,1'-cyclopropane]-12-one
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C22H20N4O2
 1
1 IC50 = 900 nM
CP0054417
3-Methoxy-7,8-dihydro-6H-5,10-dithia-8-aza-benzo[a]azulen-9-one
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C12H11NO2S2
 1
1 IC50 = 1090 nM
CP0337549
5-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)-N-propan-2-ylfuran-2-carboxamide
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C24H26ClN3O2
 1
1 IC50 = 1200 nM
CP0358095
(R)-3-Cyclopropylmethoxy-7-methyl-5,6,7,8-tetrahydro-10-thia-5,8-diaza-benzo[a]azulen-9-one
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C16H18N2O2S
 1
1 IC50 = 1320 nM
CP0298993
(R)-3-Methoxy-7-propyl-5,6,7,8-tetrahydro-10-thia-5,8-diaza-benzo[a]azulen-9-one
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C15H18N2O2S
 1
1 IC50 = 1520 nM
CP0806763
1,3-Diamino-6-(pyrrolidin-1-ylmethoxy)-9,9a-dihydro-4aH-xanthene-2-carbonitrile
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C19H20N4O2
 1
1 IC50 = 1680 nM
CP0362499
(S)-7-[(Benzyl-methyl-amino)-methyl]-3-methoxy-5,6,7,8-tetrahydro-10-thia-5,8-diaza-benzo[a]azulen-9-one
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C21H23N3O2S
 1
1 IC50 = 1910 nM
CP0333166
5-(4-chlorophenyl)-N-[4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl]furan-2-carboxamide
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C22H19ClN2O2
 1
1 IC50 = 2100 nM
CP0298998
((R)-7-Methyl-9-oxo-6,7,8,9-tetrahydro-5H-10-thia-5,8-diaza-benzo[a]azulen-3-yloxy)-acetic acid methyl ester
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C15H16N2O4S
 1
1 IC50 = 3440 nM
CP0066029
5-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C21H20ClN3O2
 2
1 IC50 = 5000 nM
2 IC50 = 5500 nM
CP0156227
5-(4-chloro-2-methylphenyl)-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C22H22ClN3O2
 1
1 IC50 = 5900 nM
CP0327715
5-(4-chlorophenyl)-N-[4-(4-methyl-1-piperazinyl)phenyl]-2-furancarboxamide
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C22H22ClN3O2
 1
1 IC50 = 6000 nM
CP0156229
5-(4-chlorophenyl)-N-(3-fluoro-4-piperazin-1-ylphenyl)furan-2-carboxamide
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C21H19ClFN3O2
 1
1 IC50 = 6700 nM
CP0066023
5-(5-chlorothiophen-2-yl)-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C19H18ClN3O2S
 1
1 IC50 = 6900 nM
CP0536680
5-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)-1,2-oxazole-3-carboxamide
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C20H19ClN4O2
 1
1 IC50 = 7500 nM
CP0327714
5-(2,4-dichlorophenyl)-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C21H19Cl2N3O2
 1
1 IC50 = 7600 nM
CP0360901
5-(2-chlorophenyl)-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C21H20ClN3O2
 1
1 IC50 = 8000 nM
CP0536679
5-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)thiophene-2-carboxamide
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C21H20ClN3OS
 1
1 IC50 = 9000 nM
CP0360905
2-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)-1,3-thiazole-4-carboxamide
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C20H19ClN4OS
 1
1 IC50 = 9500 nM
CP0548177
6-(4-chlorophenyl)-N-(4-piperazin-1-ylphenyl)pyridine-2-carboxamide
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C22H21ClN4O
 1
1 IC50 = 11000 nM
CP0360904
N-(4-piperazin-1-ylphenyl)-5-[4-(trifluoromethyl)phenyl]furan-2-carboxamide
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C22H20F3N3O2
 1
1 IC50 = 20000 nM
CP0111164
5-(4-methoxyphenyl)-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C22H23N3O3
 1
1 IC50 = 22000 nM
CP0066024
5-(4-chlorophenyl)-N-[4-piperazin-1-yl-2-(trifluoromethyl)phenyl]furan-2-carboxamide
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C22H19ClF3N3O2
 1
1 IC50 > 20000 nM
CP0417358
5-(3-chlorophenyl)-N-(4-piperazin-1-ylphenyl)furan-2-carboxamide
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C21H20ClN3O2
 1
1 IC50 > 20000 nM
Clinical Information about the Protein
Target 1 ( MAPK-activated protein kinase 2 (MAPKAPK2) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Psoriatic arthritis [ICD-11: FA21]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 Zunsemetinib Phase 2
Psoriatic arthritis