General Information of the Protein
Protein ID
PT05364
Protein Name
Heat shock factor protein 1
Secondarily
Protein Name
Heat shock transcription factor 1
Gene Name
HSF1
Secondarily
Gene Name
HSTF1
Sequence
MDLPVGPGAAGPSNVPAFLTKLWTLVSDPDTDALICWSPSGNSFHVFDQGQFAKEVLPKYFKHNNMASFVRQLNMYGFRKVVHIEQGGLVKPERDDTEFQHPCFLRGQEQLLENIKRKVTSVSTLKSEDIKIRQDSVTKLLTDVQLMKGKQECMDSKLLAMKHENEALWREVASLRQKHAQQQKVVNKLIQFLISLVQSNRILGVKRKIPLMLNDSGSAHSMPKYSRQFSLEHVHGSGPYSAPSPAYSSSSLYAPDAVASSGPIISDITELAPASPMASPGGSIDERPLSSSPLVRVKEEPPSPPQSPRVEEASPGRPSSVDTLLSPTALIDSILRESEPAPASVTALTDARGHTDTEGRPPSPPPTSTPEKCLSVACLDKNELSDHLDAMDSNLDNLQTMLSSHGFSVDTSALLDLFSPSVTVPDMSLPDLDSSLASIQELLSPQEPPRPPEAENSSPDSGKQLVHYTAQPLFLLDPGSVDTGSNDLPVLFELGEGSYFSEGDGFAEDPTISLLTGSEPPKAKDPTVS
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Organism
Homo sapiens, Human
Protein Classification
Other cytosolic protein
Function
Functions as a stress-inducible and DNA-binding transcription factor that plays a central role in the transcriptional activation of the heat shock response (HSR), leading to the expression of a large class of molecular chaperones, heat shock proteins (HSPs), that protect cells from cellular insult damage (PubMed:1871105, PubMed:11447121, PubMed:1986252, PubMed:7760831, PubMed:7623826, PubMed:8946918, PubMed:8940068, PubMed:9341107, PubMed:9121459, PubMed:9727490, PubMed:9499401, PubMed:9535852, PubMed:12659875, PubMed:12917326, PubMed:15016915, PubMed:25963659, PubMed:26754925, PubMed:18451878). In unstressed cells, is present in a HSP90-containing multichaperone complex that maintains it in a non-DNA-binding inactivated monomeric form (PubMed:9727490, PubMed:11583998, PubMed:16278218). Upon exposure to heat and other stress stimuli, undergoes homotrimerization and activates HSP gene transcription through binding to site-specific heat shock elements (HSEs) present in the promoter regions of HSP genes (PubMed:1871105, PubMed:1986252, PubMed:8455624, PubMed:7935471, PubMed:7623826, PubMed:8940068, PubMed:9727490, PubMed:9499401, PubMed:10359787, PubMed:11583998, PubMed:12659875, PubMed:16278218, PubMed:25963659, PubMed:26754925). Upon heat shock stress, forms a chromatin-associated complex with TTC5/STRAP and p300/EP300 to stimulate HSR transcription, therefore increasing cell survival (PubMed:18451878). Activation is reversible, and during the attenuation and recovery phase period of the HSR, returns to its unactivated form (PubMed:11583998, PubMed:16278218). Binds to inverted 5'-NGAAN-3' pentamer DNA sequences (PubMed:1986252, PubMed:26727489). Binds to chromatin at heat shock gene promoters (PubMed:25963659). Activates transcription of transcription factor FOXR1 which in turn activates transcription of the heat shock chaperones HSPA1A and HSPA6 and the antioxidant NADPH-dependent reductase DHRS2 (PubMed:34723967). Also serves several other functions independently of its transcriptional activity. Involved in the repression of Ras-induced transcriptional activation of the c-fos gene in heat-stressed cells (PubMed:9341107). Positively regulates pre-mRNA 3'-end processing and polyadenylation of HSP70 mRNA upon heat-stressed cells in a symplekin (SYMPK)-dependent manner (PubMed:14707147). Plays a role in nuclear export of stress-induced HSP70 mRNA (PubMed:17897941). Plays a role in the regulation of mitotic progression (PubMed:18794143). Also plays a role as a negative regulator of non-homologous end joining (NHEJ) repair activity in a DNA damage-dependent manner (PubMed:26359349). Involved in stress-induced cancer cell proliferation in a IER5-dependent manner (PubMed:26754925).
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Uniprot ID
Primary ID:
Q00613

Secondarily ID:
A8K4L0
A8MW26
Q53XT4
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Ensembl ID
ENSG00000185122
HGNC ID
HGNC:5224
Subcellular Location
Nucleus
Cytoplasm
Nucleus
Nucleoplasm
Cytoplasm
Perinuclear region
Cytoplasm
Cytoskeleton
Spindle pole
Cytoplasm
Cytoskeleton
Microtubule organizing center
Centrosome
Chromosome
Centromere
Kinetochore
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: CL000017 , HeLa
Compound ID Compound Name Compound Formula
CP0093591
(2R,4aS,6aR,6aS,14aS,14bR)-10-hydroxy-2,4a,6a,6a,9,14a-hexamethyl-11-oxo-1,3,4,5,6,13,14,14b-octahydropicene-2-carboxylic acid
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C29H38O4
 2
1
EC50 = 1100 nM
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2
EC50 = 2600 nM
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CP0439330
3-(benzo[d]thiazol-2-yl)-1-isobutyl-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
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C17H16N6O2S
 1
1
EC50 = 1300 nM
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CP0418141
1-butyl-6-methyl-3-(thiazol-2-yl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
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C13H14N6O2S
 1
1
EC50 = 2100 nM
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CP0429671
3-(benzo[d]thiazol-2-yl)-1-butyl-6-methylpyrimido[4,5-c]pyridazine-5,7(1H,6H)-dione
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C17H16N6O2S
 1
1
EC50 = 2500 nM
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CP0439328
3-(benzo[d]thiazol-2-yl)-1-isopentyl-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
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C18H18N6O2S
 1
1
EC50 = 2500 nM
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CP0506355
1-butyl-6-methyl-3-(quinolin-2-yl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
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C19H18N6O2
 1
1
EC50 = 2500 nM
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CP0474640
3-(benzo[d]thiazol-2-yl)-1-benzyl-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
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C20H14N6O2S
 1
1
EC50 = 4100 nM
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CP0209125
1-Ethyl-6-methyl-3-thiophen-2-yl-1H-pyrimido[5,4-e][1,2,4]triazine-5,7-dione
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C12H11N5O2S
 1
1
EC50 = 5100 nM
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CP0496181
1-butyl-3-(1H-imidazol-2-yl)-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
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C13H15N7O2
 1
1
EC50 = 7700 nM
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CP0429669
1-butyl-6-methyl-3-(5-methylthiophen-2-yl)-5,7-dioxo-1,5,6,7-tetrahydropyrimido[5,4-e][1,2,4]triazine 4-oxide
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C15H17N5O3S
 1
1
EC50 = 8600 nM
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CP0514658
1-butyl-6-methyl-3-(5-methylfuran-2-yl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
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C15H17N5O3
 1
1
EC50 = 9900 nM
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CP0431034
1-butyl-6-methyl-3-(5-methylfuran-2-yl)-5,7-dioxo-1,5,6,7-tetrahydropyrimido[5,4-e][1,2,4]triazine 4-oxide
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C15H17N5O4
 1
1
EC50 = 10000 nM
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CP0431031
1-ethyl-3-(furan-2-yl)-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
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C12H11N5O3
 1
1
EC50 = 10100 nM
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CP0496180
1-ethyl-6-methyl-3-(5-methylthiophen-2-yl)-5,7-dioxo-1,5,6,7-tetrahydropyrimido[5,4-e][1,2,4]triazine 4-oxide
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C13H13N5O3S
 1
1
EC50 = 11600 nM
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CP0509654
(2Z)-N-(2-hydroxy-3-piperidin-1-ylpropoxy)benzo[e][1,3]benzoxazole-2-carboximidoyl chloride
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C20H22ClN3O3
 1
1
EC50 = 12100 nM
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CP0407549
(2Z)-N-[3-[cyclopropylmethyl(propan-2-yl)amino]-2-hydroxypropoxy]-1,3-benzoxazole-2-carboximidoyl chloride
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C18H24ClN3O3
 1
1
EC50 = 12400 nM
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CP0401009
3-(benzo[d]thiazol-2-yl)-1-(4-fluorobenzyl)-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
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C20H13FN6O2S
 1
1
EC50 = 14000 nM
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CP0401010
1-butyl-6-methyl-3-phenylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
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C16H17N5O2
 1
1
EC50 = 14800 nM
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CP0429670
1-butyl-6-methyl-5,7-dioxo-3-(1H-pyrrol-2-yl)-1,5,6,7-tetrahydropyrimido[5,4-e][1,2,4]triazine 4-oxide
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C14H16N6O3
 1
1
EC50 = 14900 nM
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CP0407550
(2Z)-N-[3-[tert-butyl(propan-2-yl)amino]-2-hydroxypropoxy]-1,3-benzoxazole-2-carboximidoyl chloride
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C18H26ClN3O3
 1
1
EC50 = 16600 nM
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CP0496196
1-butyl-6-methyl-3-(5-methylthiophen-2-yl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
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C15H17N5O2S
 1
1
EC50 = 16800 nM
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CP0454257
1-ethyl-6-methyl-3-(5-methylthiophen-2-yl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
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C13H13N5O2S
 1
1
EC50 = 17300 nM
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CP0474588
(2Z)-N-[3-(3,5-dimethylpiperidin-1-yl)-2-hydroxypropoxy]-1,3-benzoxazole-2-carboximidoyl chloride
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C18H24ClN3O3
 1
1
EC50 = 17400 nM
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CP0407534
7-fluoro-N-(2-hydroxy-3-(piperidin-1-yl)propoxy)benzo[d]oxazole-2-carbimidoyl chloride
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C16H19ClFN3O3
 1
1
EC50 = 18500 nM
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CP0506150
4-fluoro-N-(2-hydroxy-3-(piperidin-1-yl)propoxy)benzo[d]oxazole-2-carbimidoyl chloride
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C16H19ClFN3O3
 1
1
EC50 = 20200 nM
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CP0431030
1-ethyl-6-methyl-3-(5-methylfuran-2-yl)-5,7-dioxo-1,5,6,7-tetrahydropyrimido[5,4-e][1,2,4]triazine 4-oxide
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C13H13N5O4
 1
1
EC50 = 20600 nM
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CP0498728
(2Z)-N-[3-(dibutylamino)-2-hydroxypropoxy]-1,3-benzoxazole-2-carboximidoyl chloride
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C19H28ClN3O3
 1
1
EC50 = 20900 nM
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CP0524220
5-chloro-N-(2-hydroxy-3-(piperidin-1-yl)propoxy)benzo[d]oxazole-2-carbimidoyl chloride
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C16H19Cl2N3O3
 1
1
EC50 = 20900 nM
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CP0504000
(2Z)-N-[3-[3-fluoropropyl(propan-2-yl)amino]-2-hydroxypropoxy]-1,3-benzoxazole-2-carboximidoyl chloride
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C17H23ClFN3O3
 1
1
EC50 = 22800 nM
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CP0387577
6-chloro-N-(2-hydroxy-3-(piperidin-1-yl)propoxy)benzo[d]oxazole-2-carbimidoyl chloride
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C16H19Cl2N3O3
 1
1
EC50 = 22900 nM
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CP0427352
(2Z)-N-[3-[ethyl(propyl)amino]-2-hydroxypropoxy]-1,3-benzoxazole-2-carboximidoyl chloride
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C16H22ClN3O3
 1
1
EC50 = 23000 nM
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CP0503992
(2Z)-N-[3-(dipropylamino)-2-hydroxypropoxy]-1,3-benzoxazole-2-carboximidoyl chloride
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C17H24ClN3O3
 1
1
EC50 = 23900 nM
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CP0919772
N-(2-hydroxy-3-(isopropyl(propyl)amino)propoxy)benzo[d]oxazole-2-carbimidoyl chloride
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C17H24ClN3O3
 1
1
EC50 = 24100 nM
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CP0431038
1-ethyl-6-methyl-5,7-dioxo-3-(1H-pyrrol-2-yl)-1,5,6,7-tetrahydropyrimido[5,4-e][1,2,4]triazine 4-oxide
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C12H12N6O3
 1
1
EC50 = 24700 nM
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CP0387580
(2Z)-N-[3-[di(propan-2-yl)amino]-2-hydroxypropoxy]-1,3-benzoxazole-2-carboximidoyl chloride
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C17H24ClN3O3
 1
1
EC50 = 25500 nM
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CP0372549
(2Z)-N-[3-(diethylamino)-2-hydroxypropoxy]-1,3-benzoxazole-2-carboximidoyl chloride
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C15H20ClN3O3
 1
1
EC50 = 27100 nM
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CP0471685
(Z,2R)-6-(1,3-benzoxazol-2-yl)-6-chloro-1-[propan-2-yl(propyl)amino]hex-5-en-2-ol
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C19H27ClN2O2
 1
1
EC50 = 28600 nM
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CP0509635
(2Z)-N-[2-hydroxy-3-[2-hydroxyethyl(propan-2-yl)amino]propoxy]-1,3-benzoxazole-2-carboximidoyl chloride
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C16H22ClN3O4
 1
1
EC50 = 28700 nM
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CP0514117
6-fluoro-N-(2-hydroxy-3-(piperidin-1-yl)propoxy)benzo[d]oxazole-2-carbimidoyl chloride
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C16H19ClFN3O3
 1
1
EC50 = 29400 nM
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CP0427355
(2Z)-N-(2-hydroxy-3-piperidin-1-ylpropoxy)-6-methyl-1,3-benzoxazole-2-carboximidoyl chloride
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C17H22ClN3O3
 1
1
EC50 = 31000 nM
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CP0504815
(Z,2S)-6-(1,3-benzoxazol-2-yl)-6-chloro-1-[propan-2-yl(propyl)amino]hex-5-en-2-ol
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C19H27ClN2O2
 1
1
EC50 = 31900 nM
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CP0407532
(2Z)-N-[3-(2,6-dimethylpiperidin-1-yl)-2-hydroxypropoxy]-1,3-benzoxazole-2-carboximidoyl chloride
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C18H24ClN3O3
 1
1
EC50 = 32400 nM
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CP0498237
1-ethyl-6-methyl-3-(1H-pyrrol-2-yl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
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C12H12N6O2
 1
1
EC50 = 35000 nM
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CP0398971
1-ethyl-3-(1H-imidazol-2-yl)-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
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C11H11N7O2
 1
1
EC50 = 39800 nM
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CP0431039
3-(1H-benzo[d]imidazol-2-yl)-1-butyl-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
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C17H17N7O2
 1
1
EC50 = 40800 nM
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CP0438801
(2Z)-N-(2-hydroxy-3-piperidin-1-ylpropoxy)-5-methyl-1,3-benzoxazole-2-carboximidoyl chloride
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C17H22ClN3O3
 1
1
EC50 = 41600 nM
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CP0506151
6-(N,N-dimethylsulfamoyl)-N-(2-hydroxy-3-(piperidin-1-yl)propoxy)benzo[d]oxazole-2-carbimidoyl chloride
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C18H25ClN4O5S
 1
1
EC50 = 41600 nM
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CP0498383
(2Z)-N-(2-hydroxy-3-piperidin-1-ylpropoxy)-1,3-benzoxazole-2-carboximidoyl chloride
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C16H20ClN3O3
 1
1
EC50 = 41700 nM
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CP0407536
5-(ethylsulfonyl)-N-(2-hydroxy-3-(piperidin-1-yl)propoxy)benzo[d]oxazole-2-carbimidoyl chloride
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C18H24ClN3O5S
 1
1
EC50 = 42900 nM
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CP0491210
1-ethyl-6-methyl-3-(5-methylfuran-2-yl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
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C13H13N5O3
 1
1
EC50 = 46300 nM
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CP0407533
5-fluoro-N-(2-hydroxy-3-(piperidin-1-yl)propoxy)benzo[d]oxazole-2-carbimidoyl chloride
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C16H19ClFN3O3
 1
1
EC50 = 51300 nM
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CP0427354
(2Z)-N-(2-hydroxy-3-piperidin-1-ylpropoxy)-1,3-benzothiazole-2-carboximidoyl chloride
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C16H20ClN3O2S
 1
1
EC50 = 52600 nM
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CP0498384
(2Z)-N-[3-(3-fluoropiperidin-1-yl)-2-hydroxypropoxy]-1,3-benzoxazole-2-carboximidoyl chloride
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C16H19ClFN3O3
 1
1
EC50 = 52600 nM
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CP0504814
(2Z)-N-(2-hydroxy-3-pyrrolidin-1-ylpropoxy)-1,3-benzothiazole-2-carboximidoyl chloride
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C15H18ClN3O2S
 1
1
EC50 = 62800 nM
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