General Information of the Protein
Protein ID
PT02289
Protein Name
Serine/threonine-protein kinase/endoribonuclease IRE1
Secondarily
Protein Name
Endoplasmic reticulum-to-nucleus signaling 1
Inositol-requiring protein 1
Ire1-alpha
Gene Name
ERN1
Secondarily
Gene Name
IRE1
Sequence
MPARRLLLLLTLLLPGLGIFGSTSTVTLPETLLFVSTLDGSLHAVSKRTGSIKWTLKEDPVLQVPTHVEEPAFLPDPNDGSLYTLGSKNNEGLTKLPFTIPELVQASPCRSSDGILYMGKKQDIWYVIDLLTGEKQQTLSSAFADSLCPSTSLLYLGRTEYTITMYDTKTRELRWNATYFDYAASLPEDDVDYKMSHFVSNGDGLVVTVDSESGDVLWIQNYASPVVAFYVWQREGLRKVMHINVAVETLRYLTFMSGEVGRITKWKYPFPKETEAKSKLTPTLYVGKYSTSLYASPSMVHEGVAVVPRGSTLPLLEGPQTDGVTIGDKGECVITPSTDVKFDPGLKSKNKLNYLRNYWLLIGHHETPLSASTKMLERFPNNLPKHRENVIPADSEKKSFEEVINLVDQTSENAPTTVSRDVEEKPAHAPARPEAPVDSMLKDMATIILSTFLLIGWVAFIITYPLSMHQQQQLQHQQFQKELEKIQLLQQQQQQLPFHPPGDTAQDGELLDTSGPYSESSGTSSPSTSPRASNHSLCSGSSASKAGSSPSLEQDDGDEETSVVIVGKISFCPKDVLGHGAEGTIVYRGMFDNRDVAVKRILPECFSFADREVQLLRESDEHPNVIRYFCTEKDRQFQYIAIELCAATLQEYVEQKDFAHLGLEPITLLQQTTSGLAHLHSLNIVHRDLKPHNILISMPNAHGKIKAMISDFGLCKKLAVGRHSFSRRSGVPGTEGWIAPEMLSEDCKENPTYTVDIFSAGCVFYYVISEGSHPFGKSLQRQANILLGACSLDCLHPEKHEDVIARELIEKMIAMDPQKRPSAKHVLKHPFFWSLEKQLQFFQDVSDRIEKESLDGPIVKQLERGGRAVVKMDWRENITVPLQTDLRKFRTYKGGSVRDLLRAMRNKKHHYRELPAEVRETLGSLPDDFVCYFTSRFPHLLAHTYRAMELCSHERLFQPYYFHEPPEPQPPVTPDAL
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
Function
Serine/threonine-protein kinase and endoribonuclease that acts as a key sensor for the endoplasmic reticulum unfolded protein response (UPR) (PubMed:11175748, PubMed:11779464, PubMed:12637535, PubMed:21317875, PubMed:28128204, PubMed:9637683, PubMed:30118681). In unstressed cells, the endoplasmic reticulum luminal domain is maintained in its inactive monomeric state by binding to the endoplasmic reticulum chaperone HSPA5/BiP (PubMed:21317875). Accumulation of misfolded proteins in the endoplasmic reticulum causes release of HSPA5/BiP, allowing the luminal domain to homodimerize, promoting autophosphorylation of the kinase domain and subsequent activation of the endoribonuclease activity (PubMed:21317875). The endoribonuclease activity is specific for XBP1 mRNA and excises 26 nucleotides from XBP1 mRNA (PubMed:11779464, PubMed:24508390, PubMed:21317875). The resulting spliced transcript of XBP1 encodes a transcriptional activator protein that up-regulates expression of UPR target genes (PubMed:11779464, PubMed:24508390, PubMed:21317875). Acts as an upstream signal for ER stress-induced GORASP2-mediated unconventional (ER/Golgi-independent) trafficking of CFTR to cell membrane by modulating the expression and localization of SEC16A (PubMed:21884936, PubMed:28067262).
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Uniprot ID
Primary ID:
O75460

Secondarily ID:
A1L457
A8K8N8
A8MXS7
Q59EE2
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Ensembl ID
ENSG00000178607
HGNC ID
HGNC:3449
Subcellular Location
Endoplasmic reticulum 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: CL000006 , HEK293
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0342595
 Compound Info 
US8614253, 29-18
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C18H13NO3
  1
1
EC50 = 1000 nM
 Bioactivity Info 
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CP0325735
 Compound Info 
US8614253, 29-19
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C20H17NO3
  1
1
EC50 = 3000 nM
 Bioactivity Info 
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CP0506728
 Compound Info 
US8614253, 43-76
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C15H12O4
  1
1
EC50 = 3000 nM
 Bioactivity Info 
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CP0358895
 Compound Info 
US8614253, 29-3
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C15H10N2O2
  1
1
EC50 = 4000 nM
 Bioactivity Info 
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CP0065079
 Compound Info 
US8614253, 29-2
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C16H11NO2
  1
1
EC50 = 5000 nM
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CP0216821
 Compound Info 
US8614253, 32-4
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C21H19NO3
  1
1
EC50 = 5000 nM
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CP0528991
 Compound Info 
US8614253, 29-4
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C22H19NO4
  1
1
EC50 = 5000 nM
 Bioactivity Info 
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CP0246203
 Compound Info 
US8614253, 34-1
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C10H7NO2
  1
1
EC50 = 7000 nM
 Bioactivity Info 
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CP0358896
 Compound Info 
US8614253, 29-7
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C15H10O3
  1
1
EC50 = 7000 nM
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CP0117557
 Compound Info 
US8614253, 42-3
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C11H7BrO2
  1
1
EC50 = 10000 nM
 Bioactivity Info 
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CP0173581
 Compound Info 
US8614253, 31-2
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C17H11NO4
  1
1
EC50 = 10000 nM
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CP0220215
 Compound Info 
US8614253, 29-17
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C18H13NO3
  1
1
EC50 = 10000 nM
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CP0300381
 Compound Info 
US8614253, 29-5
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C18H12O4
  1
1
EC50 = 10000 nM
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CP0346880
 Compound Info 
US8614253, 29-1
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C19H14O4
  1
1
EC50 = 10000 nM
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CP0353146
 Compound Info 
US8614253, 29-8
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C18H14O3
  1
1
EC50 = 10000 nM
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CP0359890
 Compound Info 
US8614253, 34-3
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C10H7NO2
  1
1
EC50 = 10000 nM
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CP0117458
 Compound Info 
US8614253, 29-11
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C20H13NO2
  1
1
EC50 = 15000 nM
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CP0563849
 Compound Info 
US8614253, 29-10
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C15H10O2S
  1
1
EC50 = 20000 nM
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CP0065076
 Compound Info 
US8614253, 3-6
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C11H8O2S
  1
1
EC50 = 30000 nM
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CP0114448
 Compound Info 
US8614253, 26-9
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C14H12O4S
  1
1
EC50 = 30000 nM
 Bioactivity Info 
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CP0114449
 Compound Info 
US8614253, 26-15
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C14H13NO4
  1
1
EC50 = 30000 nM
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CP0117457
 Compound Info 
US8614253, 29-9
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C17H13NO3
  1
1
EC50 = 30000 nM
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CP0117460
 Compound Info 
US8614253, 29-20
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C18H12O4
  1
1
EC50 = 30000 nM
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CP0117462
 Compound Info 
US8614253, 32-5
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C26H21NO3
  1
1
EC50 = 30000 nM
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CP0117540
 Compound Info 
US8614253, 43-7
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C12H10N2O3
  1
1
EC50 = 30000 nM
 Bioactivity Info 
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CP0117556
 Compound Info 
US8614253, 41-4
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C12H11NO4S
  1
1
EC50 = 30000 nM
 Bioactivity Info 
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CP0172115
 Compound Info 
US8614253, 43-16
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C12H10O3S
  1
1
EC50 = 30000 nM
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CP0175325
 Compound Info 
US8614253, 43-72
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C17H18N2O4
  1
1
EC50 = 30000 nM
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CP0187855
 Compound Info 
US8614253, 43-84
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C12H7F3O3
  1
1
EC50 = 30000 nM
 Bioactivity Info 
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CP0215120
 Compound Info 
US8614253, 26-6
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C13H11NO3
  1
1
EC50 = 30000 nM
 Bioactivity Info 
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CP0253457
 Compound Info 
US8614253, 43-56
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C14H11NO3
  1
1
EC50 = 30000 nM
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CP0259872
 Compound Info 
US8614253, 38-15
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C17H14N2O2S
  1
1
EC50 = 30000 nM
 Bioactivity Info 
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CP0264978
 Compound Info 
US8614253, 43-69
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C15H12O4
  1
1
EC50 = 30000 nM
 Bioactivity Info 
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CP0284285
 Compound Info 
US8614253, 26-2
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C12H12N2O3
  1
1
EC50 = 30000 nM
 Bioactivity Info 
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CP0325733
 Compound Info 
US8614253, 29-12
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C20H13NO2
  1
1
EC50 = 30000 nM
 Bioactivity Info 
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CP0331110
 Compound Info 
US8614253, 38-7
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C14H15NO3S
  1
1
EC50 = 30000 nM
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CP0361764
 Compound Info 
US8614253, 43-27
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C12H10O4
  1
1
EC50 = 30000 nM
 Bioactivity Info 
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CP0442851
 Compound Info 
US8614253, 43-12
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C12H10O3S
  1
1
EC50 = 30000 nM
 Bioactivity Info 
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CP0114458
 Compound Info 
US8614253, 43-79
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C19H19NO3
  1
1
EC50 = 50000 nM
 Bioactivity Info 
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CP0117446
 Compound Info 
US8614253, 43-60
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C14H11NO3
  1
1
EC50 = 50000 nM
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CP0123214
 Compound Info 
US8614253, 26-22
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C16H10FNO2
  1
1
EC50 = 50000 nM
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CP0123218
 Compound Info 
US8614253, 43-13
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C11H7NO4S
  1
1
EC50 = 50000 nM
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CP0132835
 Compound Info 
US8614253, 38-4
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C28H28N2O4S4
  1
1
EC50 = 50000 nM
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CP0132925
 Compound Info 
US8614253, 43-35
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C15H9FO2S
  1
1
EC50 = 50000 nM
 Bioactivity Info 
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CP0132934
 Compound Info 
US8614253, 32-1
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C23H21NO3
  1
1
EC50 = 50000 nM
 Bioactivity Info 
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CP0172026
 Compound Info 
US8614253, 26-14
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C17H13NO3
  1
1
EC50 = 50000 nM
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CP0172034
 Compound Info 
US8614253, 38-1
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C20H22Br2N2O4S2
  1
1
EC50 = 50000 nM
 Bioactivity Info 
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CP0172114
 Compound Info 
US8614253, 43-14
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C16H12O3S
  1
1
EC50 = 50000 nM
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CP0174354
 Compound Info 
US8614253, 26-24
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C17H10F3NO2
  1
1
EC50 = 50000 nM
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CP0216820
 Compound Info 
US8614253, 32-2
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C23H22N2O3
  1
1
EC50 = 50000 nM
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CP0240985
 Compound Info 
US8614253, 26-7
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C13H12O3S
  1
1
EC50 = 50000 nM
 Bioactivity Info 
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CP0252059
 Compound Info 
US8614253, 43-61
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C16H15NO3
  1
1
EC50 = 50000 nM
 Bioactivity Info 
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CP0252090
 Compound Info 
US8614253, 29-21
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C20H18N2O3
  1
1
EC50 = 50000 nM
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CP0259867
 Compound Info 
US8614253, 32-6
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C20H18N2O3
  1
1
EC50 = 50000 nM
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CP0259871
 Compound Info 
US8614253, 38-5
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C15H15NO2S
  1
1
EC50 = 50000 nM
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CP0324486
 Compound Info 
US9241942, 38-4
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C28H28N2O5S3
  1
1
EC50 = 50000 nM
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CP0325734
 Compound Info 
US8614253, 29-13
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C18H13FO2
  1
1
EC50 = 50000 nM
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CP0325738
 Compound Info 
US8614253, 38-2
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C16H16BrNO3
  1
1
EC50 = 50000 nM
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CP0349117
 Compound Info 
US8614253, 42-11
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C11H9NO2
  1
1
EC50 = 50000 nM
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CP0353147
 Compound Info 
US8614253, 38-3
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C11H12BrNO2
  1
1
EC50 = 50000 nM
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CP0358898
 Compound Info 
US8614253, 32-3
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C26H21NO3
  1
1
EC50 = 50000 nM
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CP0518991
 Compound Info 
US8614253, 38-6
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C20H19NO3S
  1
1
EC50 = 50000 nM
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CP0572408
 Compound Info 
US8614253, 43-58
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C15H11FO4
  1
1
EC50 = 50000 nM
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CP0117463
 Compound Info 
US8614253, 32-8
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C22H19NO4
  1
1
EC50 = 60000 nM
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CP0131865
 Compound Info 
US8614253, 32-9
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C23H23N3O4
  1
1
EC50 = 60000 nM
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CP0132931
 Compound Info 
US8614253, 43-63
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C15H11NO6
  1
1
EC50 = 60000 nM
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CP0132935
 Compound Info 
US8614253, 32-7
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C21H18N2O4
  1
1
EC50 = 60000 nM
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CP0132936
 Compound Info 
US9241942, 32-12
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C21H20N2O4
  1
1
EC50 = 60000 nM
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CP0174196
 Compound Info 
US8614253, 43-78
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C18H17NO4
  1
1
EC50 = 60000 nM
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CP0175326
 Compound Info 
US8614253, 43-73
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C14H9FO4
  1
1
EC50 = 60000 nM
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CP0175327
 Compound Info 
US8614253, 43-74
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C14H10FNO3
  1
1
EC50 = 60000 nM
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CP0175328
 Compound Info 
US8614253, 43-75
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C16H14FNO3
  1
1
EC50 = 60000 nM
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CP0226672
 Compound Info 
US8614253, 32-10
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C22H21N3O3
  1
1
EC50 = 60000 nM
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CP0265012
 Compound Info 
US9241942, 32-11
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C20H17NO5
  1
1
EC50 = 60000 nM
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CP0325465
 Compound Info 
US8614253, 41-1
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C13H11NO3
  1
1
EC50 = 60000 nM
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CP0328535
 Compound Info 
US8614253, 43-77
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C16H15NO3
  1
1
EC50 = 60000 nM
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CP0419934
 Compound Info 
US8614253, 43-59
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C14H9FO4
  1
1
EC50 = 60000 nM
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CP0123216
 Compound Info 
US8614253, 26-1
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C13H11NO3
  1
1
EC50 = 70000 nM
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CP0123217
 Compound Info 
US8614253, 3-3
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C11H7FO2S
  1
1
EC50 = 70000 nM
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CP0123234
 Compound Info 
US8614253, 42-14
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C15H11NO3
  1
1
EC50 = 70000 nM
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CP0132938
 Compound Info 
US9241942, 38-11
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C13H11N5O2S
  1
1
EC50 = 70000 nM
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CP0164710
 Compound Info 
US8614253, 26-11
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C17H13NO3
  1
1
EC50 = 70000 nM
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CP0191815
 Compound Info 
US8614253, 3-10
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C15H12O5
  1
1
EC50 = 70000 nM
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CP0216837
 Compound Info 
US8614253, 43-15
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C16H12O3S
  1
1
EC50 = 70000 nM
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CP0253455
 Compound Info 
US8614253, 3-2
   Show/Hide
C11H7NO4S
  1
1
EC50 = 70000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0328536
 Compound Info 
US8614253, 39-2
   Show/Hide
C17H19NO2
  1
1
EC50 = 70000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0359891
 Compound Info 
US8614253, 43-17
   Show/Hide
C11H8O2S
  1
1
EC50 = 70000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0412226
 Compound Info 
US8614253, 26-10
   Show/Hide
C13H10N2O5
  1
1
EC50 = 70000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0528989
 Compound Info 
US8614253, 26-13
   Show/Hide
C16H10N2O4
  1
1
EC50 = 70000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0561453
 Compound Info 
US8614253, 43-33
   Show/Hide
C12H7F3O2S
  1
1
EC50 = 70000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0318244
 Compound Info 
US9241942, 38-10
   Show/Hide
C9H8BrN5O2
  1
1
EC50 = 75000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0097648
 Compound Info 
US8614253, 3-4
   Show/Hide
C11H7FN2O2
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0107278
 Compound Info 
US8614253, 29-15
   Show/Hide
C18H13ClO2
  1
1
EC50 > 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0114452
 Compound Info 
US8614253, 43-6
   Show/Hide
C11H8N2O2
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0114456
 Compound Info 
US8614253, 43-64
   Show/Hide
C14H10N2O5
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0114457
 Compound Info 
US8614253, 43-67
   Show/Hide
C14H9NO6
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0114463
 Compound Info 
US8614253, 36-1
   Show/Hide
C11H12BrNO4S
  1
1
EC50 > 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0114753
 Compound Info 
US8614253, 36-6
   Show/Hide
C11H10BrNO5S
  1
1
EC50 > 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0114754
 Compound Info 
US8614253, 38-12
   Show/Hide
C10H12BrNO3
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0117440
 Compound Info 
US8614253, 43-23
   Show/Hide
C15H10O2S
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0117441
 Compound Info 
US8614253, 43-24
   Show/Hide
C15H10O2S
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0117442
 Compound Info 
US8614253, 43-25
   Show/Hide
C11H8O3
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0117443
 Compound Info 
US8614253, 43-26
   Show/Hide
C12H10O4
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0117445
 Compound Info 
US8614253, 43-29
   Show/Hide
C11H7NO5
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0117461
 Compound Info 
US8614253, 31-1
   Show/Hide
C18H14O4S
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0117464
 Compound Info 
US8614253, 36-8
   Show/Hide
C14H15NO2S2
  1
1
EC50 > 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0117466
 Compound Info 
US9241942, 37-3
   Show/Hide
C14H10O3S
  1
1
EC50 > 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0117559
 Compound Info 
US8614253, 36-4
   Show/Hide
C17H19NO4S2
  1
1
EC50 > 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0119918
 Compound Info 
US8614253, 26-21
   Show/Hide
C13H9FO3S
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0121352
 Compound Info 
US8614253, 43-3
   Show/Hide
C16H14O5
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0121353
 Compound Info 
US8614253, 43-18
   Show/Hide
C12H11NO3
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0123215
 Compound Info 
US8614253, 26-23
   Show/Hide
C16H10N2O4
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0123220
 Compound Info 
US8614253, 43-20
   Show/Hide
C15H12O3
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0123221
 Compound Info 
US8614253, 43-21
   Show/Hide
C15H11FO3
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0123222
 Compound Info 
US8614253, 43-28
   Show/Hide
C11H7NO5
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0123223
 Compound Info 
US8614253, 43-52
   Show/Hide
C15H11NO6
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0123231
 Compound Info 
US8614253, 38-13
   Show/Hide
C11H9BrN2O2S
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0131868
 Compound Info 
US9241942, 37-1
   Show/Hide
C14H9NO2
  1
1
EC50 > 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0132927
 Compound Info 
US8614253, 43-37
   Show/Hide
C17H17NO4
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0132929
 Compound Info 
US8614253, 43-43
   Show/Hide
C15H10F3NO3
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0132930
 Compound Info 
US8614253, 43-47
   Show/Hide
C19H16F3NO4
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0137278
 Compound Info 
US8614253, 26-16
   Show/Hide
C15H9NO4S
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0164709
 Compound Info 
US8614253, 26-5
   Show/Hide
C12H8FNO2
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0172025
 Compound Info 
US8614253, 26-8
   Show/Hide
C13H10FNO3
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0172113
 Compound Info 
US8614253, 26-27
   Show/Hide
C11H9N3O4
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0173582
 Compound Info 
US8614253, 36-2
   Show/Hide
C13H16BrNO4S
  1
1
EC50 > 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0173601
 Compound Info 
US8614253, 43-68
   Show/Hide
C14H10O4
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0174355
 Compound Info 
US8614253, 26-25
   Show/Hide
C11H10N2O3
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0174356
 Compound Info 
US8614253, 26-26
   Show/Hide
C11H9FN2O2
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0174358
 Compound Info 
US8614253, 43-40
   Show/Hide
C15H13NO4
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0187459
 Compound Info 
US8614253, 43-55
   Show/Hide
C13H10O5S
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0187888
 Compound Info 
US8614253, 43-66
   Show/Hide
C16H14N2O5
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0215124
 Compound Info 
US8614253, 43-39
   Show/Hide
C19H19NO5
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0215126
 Compound Info 
US8614253, 43-41
   Show/Hide
C15H14O5S
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0216819
 Compound Info 
US8614253, 29-14
   Show/Hide
C18H13ClO2
  1
1
EC50 > 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0216839
 Compound Info 
US8614253, 43-36
   Show/Hide
C15H13NO4
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0223460
 Compound Info 
US8614253, 26-12
   Show/Hide
C16H10FNO2
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0240984
 Compound Info 
US8614253, 3-67
   Show/Hide
C13H11NO3
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0243312
 Compound Info 
US8614253, 3-24
   Show/Hide
C16H14O4
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0246190
 Compound Info 
US8614253, 43-9
   Show/Hide
C13H13NO4
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0246191
 Compound Info 
US8614253, 43-30
   Show/Hide
C15H9NO4S
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0246192
 Compound Info 
US8614253, 43-44
   Show/Hide
C18H16N2O6
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0252054
 Compound Info 
US8614253, 26-18
   Show/Hide
C12H10FNO3
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0252055
 Compound Info 
US8614253, 26-20
   Show/Hide
C13H8F3NO2
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0252058
 Compound Info 
US8614253, 43-53
   Show/Hide
C15H12O5
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0252060
 Compound Info 
US8614253, 43-62
   Show/Hide
C14H9NO6
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0259855
 Compound Info 
US8614253, 26-3
   Show/Hide
C12H8N2O4
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0259856
 Compound Info 
US8614253, 26-4
   Show/Hide
C12H9NO2
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0259862
 Compound Info 
US8614253, 43-71
   Show/Hide
C11H8O3
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0284220
 Compound Info 
US8614253, 26-19
   Show/Hide
C11H7FO3
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0292674
 Compound Info 
US8614253, 43-49
   Show/Hide
C17H14F3NO3
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0299939
 Compound Info 
US8614253, 43-54
   Show/Hide
C15H14O5S
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0304862
 Compound Info 
US8614253, 26-17
   Show/Hide
C16H12O4
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0325737
 Compound Info 
US8614253, 36-10
   Show/Hide
C12H13Br2NO4S
  1
1
EC50 > 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0325739
 Compound Info 
US8614253, 41-2
   Show/Hide
C18H16FNO4
  1
1
EC50 > 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0325752
 Compound Info 
US8614253, 43-31
   Show/Hide
C11H7FO3
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0325753
 Compound Info 
US8614253, 43-42
   Show/Hide
C14H10FNO3
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0325754
 Compound Info 
US8614253, 43-57
   Show/Hide
C15H11FO4
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0329136
 Compound Info 
US8614253, 43-38
   Show/Hide
C17H17NO4
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0329137
 Compound Info 
US8614253, 43-51
   Show/Hide
C16H14O5
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0331095
 Compound Info 
US8614253, 43-70
   Show/Hide
C12H10N2O3
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0331096
 Compound Info 
US8614253, 43-82
   Show/Hide
C16H14FNO3
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0331107
 Compound Info 
US8614253, 36-9
   Show/Hide
C15H15NO4S2
  1
1
EC50 > 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0346710
 Compound Info 
US8614253, 43-8
   Show/Hide
C11H7N3O4
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0348262
 Compound Info 
US8614253, 36-5
   Show/Hide
C10H10BrNO3S
  1
1
EC50 > 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0358888
 Compound Info 
US8614253, 43-46
   Show/Hide
C16H14N2O5
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0358889
 Compound Info 
US8614253, 43-65
   Show/Hide
C14H10N2O5
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0359892
 Compound Info 
US8614253, 43-22
   Show/Hide
C11H7FO2S
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0370827
 Compound Info 
US8614253, 43-32
   Show/Hide
C15H9FO2S
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0412227
 Compound Info 
US8614253, 43-45
   Show/Hide
C14H11NO6S
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0469980
 Compound Info 
US8614253, 43-34
   Show/Hide
C12H9NO2
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0479228
 Compound Info 
US8614253, 43-50
   Show/Hide
C17H16O5
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0516235
 Compound Info 
US8614253, 36-3
   Show/Hide
C10H12BrNO2S
  1
1
EC50 > 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0518990
 Compound Info 
US8614253, 36-7
   Show/Hide
C14H17Br2NO4S
  1
1
EC50 > 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0557521
 Compound Info 
US8614253, 43-48
   Show/Hide
C15H12O5
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0833545
 Compound Info 
US8614253, 35-2::US9241942, 35-2
   Show/Hide
C11H9NO3
  1
1
EC50 > 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0960214
 Compound Info 
US9241942, 27-19
   Show/Hide
C13H12N2O4
  1
1
EC50 = 80000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0098253
 Compound Info 
3-(2-anilino-6-fluoro-1H-benzimidazol-5-yl)-6-chloro-N-[(1-methylpiperidin-4-yl)methyl]imidazo[1,2-b]pyridazin-8-amine
   Show/Hide
C26H26ClFN8
  3
1
IC50 = 680 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 710 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
3
IC50 = 740 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0167879
 Compound Info 
CHEMBL4565193
   Show/Hide
C25H29ClN8O2
  3
1
IC50 = 680 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 1120 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
3
IC50 = 1880 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0473260
 Compound Info 
KIRA analog, 1
   Show/Hide
C27H23F3N6O
  1
1
IC50 = 760 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0244352
 Compound Info 
3-(2-anilino-3H-benzimidazol-5-yl)-6-chloro-N-[(1-methylpiperidin-4-yl)methyl]imidazo[1,2-b]pyridazin-8-amine
   Show/Hide
C26H27ClN8
  1
1
IC50 = 890 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0167882
 Compound Info 
4-N-[6-chloro-3-(1H-indazol-5-yl)imidazo[1,2-b]pyridazin-8-yl]cyclohexane-1,4-diamine
   Show/Hide
C19H20ClN7
  1
1
IC50 = 2900 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0402830
 Compound Info 
6-chloro-N-(cyclopropylmethyl)-3-(1H-indazol-5-yl)imidazo[1,2-b]pyridazin-8-amine
   Show/Hide
C17H15ClN6
  1
1
IC50 = 4200 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000012 , Sf21
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0216821
 Compound Info 
US8614253, 32-4
   Show/Hide
C21H19NO3
  1
1 IC50 = 3 nM
CP0132936
 Compound Info 
US9241942, 32-12
   Show/Hide
C21H20N2O4
  1
1 IC50 = 5 nM
CP0220199
 Compound Info 
US8614253, 32-12
   Show/Hide
C21H20N2O3S
  1
1 IC50 = 5 nM
CP0068667
 Compound Info 
CHEMBL3356007
   Show/Hide
C32H31ClN6O3S
  2
1 IC50 = 14 nM
2 IC50 = 57 nM
CP0331110
 Compound Info 
US8614253, 38-7
   Show/Hide
C14H15NO3S
  1
1 IC50 = 15 nM
CP0132931
 Compound Info 
US8614253, 43-63
   Show/Hide
C15H11NO6
  1
1 IC50 = 21 nM
CP0065079
 Compound Info 
US8614253, 29-2
   Show/Hide
C16H11NO2
  1
1 IC50 = 23 nM
CP0518991
 Compound Info 
US8614253, 38-6
   Show/Hide
C20H19NO3S
  1
1 IC50 = 23 nM
CP0342595
 Compound Info 
US8614253, 29-18
   Show/Hide
C18H13NO3
  1
1 IC50 = 26 nM
CP0167879
 Compound Info 
CHEMBL4565193
   Show/Hide
C25H29ClN8O2
  3
1 IC50 = 27 nM
2 IC50 = 87 nM
3 IC50 = 240 nM
CP0114456
 Compound Info 
US8614253, 43-64
   Show/Hide
C14H10N2O5
  1
1 IC50 = 32 nM
CP0259871
 Compound Info 
US8614253, 38-5
   Show/Hide
C15H15NO2S
  1
1 IC50 = 34 nM
CP0117540
 Compound Info 
US8614253, 43-7
   Show/Hide
C12H10N2O3
  1
1 IC50 = 39 nM
CP0256676
 Compound Info 
4-amino-N-[6-chloro-2-fluoro-3-[(2-fluorophenyl)sulfonylamino]phenyl]-6-(1,3-dimethylpyrazol-4-yl)quinazoline-8-carboxamide
   Show/Hide
C26H20ClF2N7O3S
  1
1 IC50 = 44 nM
CP0119918
 Compound Info 
US8614253, 26-21
   Show/Hide
C13H9FO3S
  1
1 IC50 = 46 nM
CP0325753
 Compound Info 
US8614253, 43-42
   Show/Hide
C14H10FNO3
  1
1 IC50 = 46 nM
CP0259867
 Compound Info 
US8614253, 32-6
   Show/Hide
C20H18N2O3
  1
1 IC50 = 47 nM
CP0256674
 Compound Info 
4-amino-N-[6-chloro-3-[(2-chlorophenyl)sulfonylamino]-2-fluorophenyl]-6-(1,3-dimethylpyrazol-4-yl)quinazoline-8-carboxamide
   Show/Hide
C26H20Cl2FN7O3S
  1
1 IC50 = 48 nM
CP0361764
 Compound Info 
US8614253, 43-27
   Show/Hide
C12H10O4
  2
1 IC50 = 51 nM
2 IC50 = 61 nM
CP0358889
 Compound Info 
US8614253, 43-65
   Show/Hide
C14H10N2O5
  2
1 IC50 = 54 nM
2 IC50 = 154 nM
CP0358895
 Compound Info 
US8614253, 29-3
   Show/Hide
C15H10N2O2
  1
1 IC50 = 66 nM
CP0117463
 Compound Info 
US8614253, 32-8
   Show/Hide
C22H19NO4
  1
1 IC50 = 67 nM
CP0167882
 Compound Info 
CHEMBL4444939
   Show/Hide
C19H20ClN7
  3
1 IC50 = 72 nM
2 IC50 = 110 nM
3 IC50 = 320 nM
CP0114449
 Compound Info 
US8614253, 26-15
   Show/Hide
C14H13NO4
  1
1 IC50 = 74 nM
CP0359892
 Compound Info 
US8614253, 43-22
   Show/Hide
C11H7FO2S
  1
1 IC50 = 74 nM
CP0528991
 Compound Info 
US8614253, 29-4
   Show/Hide
C22H19NO4
  1
1 IC50 = 74 nM
CP0300381
 Compound Info 
US8614253, 29-5
   Show/Hide
C18H12O4
  1
1 IC50 = 79 nM
CP0098253
 Compound Info 
3-(2-anilino-6-fluoro-1H-benzimidazol-5-yl)-6-chloro-N-[(1-methylpiperidin-4-yl)methyl]imidazo[1,2-b]pyridazin-8-amine
   Show/Hide
C26H26ClFN8
  3
1 IC50 = 80 nM
2 IC50 = 160 nM
3 IC50 = 270 nM
CP0117445
 Compound Info 
US8614253, 43-29
   Show/Hide
C11H7NO5
  1
1 IC50 = 81 nM
CP0216839
 Compound Info 
US8614253, 43-36
   Show/Hide
C15H13NO4
  1
1 IC50 = 82 nM
CP0304862
 Compound Info 
US8614253, 26-17
   Show/Hide
C16H12O4
  1
1 IC50 = 82 nM
CP0175327
 Compound Info 
US8614253, 43-74
   Show/Hide
C14H10FNO3
  1
1 IC50 = 85 nM
CP0325752
 Compound Info 
US8614253, 43-31
   Show/Hide
C11H7FO3
  1
1 IC50 = 88 nM
CP0244352
 Compound Info 
3-(2-anilino-3H-benzimidazol-5-yl)-6-chloro-N-[(1-methylpiperidin-4-yl)methyl]imidazo[1,2-b]pyridazin-8-amine
   Show/Hide
C26H27ClN8
  3
1 IC50 = 90 nM
2 IC50 = 130 nM
3 IC50 = 390 nM
CP0114448
 Compound Info 
US8614253, 26-9
   Show/Hide
C14H12O4S
  1
1 IC50 = 97 nM
CP0172026
 Compound Info 
US8614253, 26-14
   Show/Hide
C17H13NO3
  1
1 IC50 = 100 nM
CP0226345
 Compound Info 
US9040714, 167
   Show/Hide
C18H19NO7
  1
1 IC50 < 100 nM
CP0114457
 Compound Info 
US8614253, 43-67
   Show/Hide
C14H9NO6
  1
1 IC50 = 101 nM
CP0123214
 Compound Info 
US8614253, 26-22
   Show/Hide
C16H10FNO2
  1
1 IC50 = 104 nM
CP0325465
 Compound Info 
US8614253, 41-1
   Show/Hide
C13H11NO3
  1
1 IC50 = 108 nM
CP0353147
 Compound Info 
US8614253, 38-3
   Show/Hide
C11H12BrNO2
  1
1 IC50 = 110 nM
CP0117443
 Compound Info 
US8614253, 43-26
   Show/Hide
C12H10O4
  1
1 IC50 = 114 nM
CP0362667
 Compound Info 
CHEMBL4781285
   Show/Hide
C25H23Cl2FN6O3S2
  1
1 IC50 = 120 nM
CP0325735
 Compound Info 
US8614253, 29-19
   Show/Hide
C20H17NO3
  1
1 IC50 = 125 nM
CP0117556
 Compound Info 
US8614253, 41-4
   Show/Hide
C12H11NO4S
  1
1 IC50 = 128 nM
CP0253457
 Compound Info 
US8614253, 43-56
   Show/Hide
C14H11NO3
  1
1 IC50 = 131 nM
CP0252060
 Compound Info 
US8614253, 43-62
   Show/Hide
C14H9NO6
  1
1 IC50 = 132 nM
CP0469980
 Compound Info 
US8614253, 43-34
   Show/Hide
C12H9NO2
  1
1 IC50 = 141 nM
CP0252059
 Compound Info 
US8614253, 43-61
   Show/Hide
C16H15NO3
  1
1 IC50 = 147 nM
CP0259856
 Compound Info 
US8614253, 26-4
   Show/Hide
C12H9NO2
  1
1 IC50 = 147 nM
CP0215120
 Compound Info 
US8614253, 26-6
   Show/Hide
C13H11NO3
  1
1 IC50 = 149 nM
CP0573865
 Compound Info 
4-amino-N-[6-chloro-3-[(2,5-difluorophenyl)sulfonylamino]-2-fluorophenyl]-6-(1,3-dimethylpyrazol-4-yl)quinazoline-8-carboxamide
   Show/Hide
C26H19ClF3N7O3S
  1
1 IC50 = 150 nM
CP0114754
 Compound Info 
US8614253, 38-12
   Show/Hide
C10H12BrNO3
  1
1 IC50 = 154 nM
CP0131868
 Compound Info 
US9241942, 37-1
   Show/Hide
C14H9NO2
  1
1 IC50 = 155 nM
CP0216820
 Compound Info 
US8614253, 32-2
   Show/Hide
C23H22N2O3
  1
1 IC50 = 157 nM
CP0132938
 Compound Info 
US9241942, 38-11
   Show/Hide
C13H11N5O2S
  1
1 IC50 = 157 nM
CP0265012
 Compound Info 
US9241942, 32-11
   Show/Hide
C20H17NO5
  1
1 IC50 = 157 nM
CP0329136
 Compound Info 
US8614253, 43-38
   Show/Hide
C17H17NO4
  1
1 IC50 = 162 nM
CP0164709
 Compound Info 
US8614253, 26-5
   Show/Hide
C12H8FNO2
  1
1 IC50 = 163 nM
CP0174354
 Compound Info 
US8614253, 26-24
   Show/Hide
C17H10F3NO2
  1
1 IC50 = 164 nM
CP0172025
 Compound Info 
US8614253, 26-8
   Show/Hide
C13H10FNO3
  1
1 IC50 = 168 nM
CP0114452
 Compound Info 
US8614253, 43-6
   Show/Hide
C11H8N2O2
  1
1 IC50 = 170 nM
CP0246203
 Compound Info 
US8614253, 34-1
   Show/Hide
C10H7NO2
  1
1 IC50 = 170 nM
CP0174358
 Compound Info 
US8614253, 43-40
   Show/Hide
C15H13NO4
  1
1 IC50 = 173 nM
CP0284220
 Compound Info 
US8614253, 26-19
   Show/Hide
C11H7FO3
  1
1 IC50 = 190 nM
CP0329137
 Compound Info 
US8614253, 43-51
   Show/Hide
C16H14O5
  1
1 IC50 = 192 nM
CP0117446
 Compound Info 
US8614253, 43-60
   Show/Hide
C14H11NO3
  1
1 IC50 = 197 nM
CP0172115
 Compound Info 
US8614253, 43-16
   Show/Hide
C12H10O3S
  1
1 IC50 = 199 nM
CP0325754
 Compound Info 
US8614253, 43-57
   Show/Hide
C15H11FO4
  1
1 IC50 = 213 nM
CP0175326
 Compound Info 
US8614253, 43-73
   Show/Hide
C14H9FO4
  1
1 IC50 = 214 nM
CP0325738
 Compound Info 
US8614253, 38-2
   Show/Hide
C16H16BrNO3
  1
1 IC50 = 221 nM
CP0325739
 Compound Info 
US8614253, 41-2
   Show/Hide
C18H16FNO4
  1
1 IC50 = 221 nM
CP0123222
 Compound Info 
US8614253, 43-28
   Show/Hide
C11H7NO5
  1
1 IC50 = 223 nM
CP0259862
 Compound Info 
US8614253, 43-71
   Show/Hide
C11H8O3
  1
1 IC50 = 223 nM
CP0187459
 Compound Info 
US8614253, 43-55
   Show/Hide
C13H10O5S
  1
1 IC50 = 230 nM
CP0132929
 Compound Info 
US8614253, 43-43
   Show/Hide
C15H10F3NO3
  1
1 IC50 = 235 nM
CP0174356
 Compound Info 
US8614253, 26-26
   Show/Hide
C11H9FN2O2
  1
1 IC50 = 236 nM
CP0362666
 Compound Info 
4-amino-N-[6-chloro-3-[(2,5-difluorophenyl)sulfonylamino]-2-fluorophenyl]-6-(1-methylpyrazol-4-yl)quinazoline-8-carboxamide
   Show/Hide
C25H17ClF3N7O3S
  1
1 IC50 = 280 nM
CP0473260
 Compound Info 
KIRA analog, 1
   Show/Hide
C27H23F3N6O
  3
1 IC50 = 290 nM
2 IC50 = 400 nM
3 IC50 = 450 nM
CP0123234
 Compound Info 
US8614253, 42-14
   Show/Hide
C15H11NO3
  1
1 IC50 = 303 nM
CP0402830
 Compound Info 
6-chloro-N-(cyclopropylmethyl)-3-(1H-indazol-5-yl)imidazo[1,2-b]pyridazin-8-amine
   Show/Hide
C17H15ClN6
  3
1 IC50 = 303 nM
2 IC50 = 1600 nM
3 IC50 = 8900 nM
CP0223460
 Compound Info 
US8614253, 26-12
   Show/Hide
C16H10FNO2
  1
1 IC50 = 305 nM
CP0174355
 Compound Info 
US8614253, 26-25
   Show/Hide
C11H10N2O3
  1
1 IC50 = 310 nM
CP0486630
 Compound Info 
CHEMBL4786638
   Show/Hide
C25H22ClF3N6O3S2
  1
1 IC50 = 320 nM
CP0346710
 Compound Info 
US8614253, 43-8
   Show/Hide
C11H7N3O4
  1
1 IC50 = 331 nM
CP0528989
 Compound Info 
US8614253, 26-13
   Show/Hide
C16H10N2O4
  2
1 IC50 = 333 nM
2 IC50 = 3333 nM
CP0412226
 Compound Info 
US8614253, 26-10
   Show/Hide
C13H10N2O5
  1
1 IC50 = 346 nM
CP0132930
 Compound Info 
US8614253, 43-47
   Show/Hide
C19H16F3NO4
  1
1 IC50 = 348 nM
CP0264978
 Compound Info 
US8614253, 43-69
   Show/Hide
C15H12O4
  1
1 IC50 = 351 nM
CP0442851
 Compound Info 
US8614253, 43-12
   Show/Hide
C12H10O3S
  1
1 IC50 = 351 nM
CP0175325
 Compound Info 
US8614253, 43-72
   Show/Hide
C17H18N2O4
  1
1 IC50 = 367 nM
CP0173601
 Compound Info 
US8614253, 43-68
   Show/Hide
C14H10O4
  1
1 IC50 = 371 nM
CP0215126
 Compound Info 
US8614253, 43-41
   Show/Hide
C15H14O5S
  1
1 IC50 = 379 nM
CP0123221
 Compound Info 
US8614253, 43-21
   Show/Hide
C15H11FO3
  1
1 IC50 = 381 nM
CP0226672
 Compound Info 
US8614253, 32-10
   Show/Hide
C22H21N3O3
  1
1 IC50 = 389 nM
CP0554623
 Compound Info 
CHEMBL4760343
   Show/Hide
C26H27Cl2FN6O3S2
  1
1 IC50 = 390 nM
CP0114458
 Compound Info 
US8614253, 43-79
   Show/Hide
C19H19NO3
  1
1 IC50 = 398 nM
CP0123218
 Compound Info 
US8614253, 43-13
   Show/Hide
C11H7NO4S
  1
1 IC50 = 401 nM
CP0358888
 Compound Info 
US8614253, 43-46
   Show/Hide
C16H14N2O5
  1
1 IC50 = 410 nM
CP0132927
 Compound Info 
US8614253, 43-37
   Show/Hide
C17H17NO4
  1
1 IC50 = 413 nM
CP0246191
 Compound Info 
US8614253, 43-30
   Show/Hide
C15H9NO4S
  1
1 IC50 = 420 nM
CP0328535
 Compound Info 
US8614253, 43-77
   Show/Hide
C16H15NO3
  1
1 IC50 = 420 nM
CP0506728
 Compound Info 
US8614253, 43-76
   Show/Hide
C15H12O4
  1
1 IC50 = 421 nM
CP0117442
 Compound Info 
US8614253, 43-25
   Show/Hide
C11H8O3
  1
1 IC50 = 441 nM
CP0331096
 Compound Info 
US8614253, 43-82
   Show/Hide
C16H14FNO3
  1
1 IC50 = 455 nM
CP0132925
 Compound Info 
US8614253, 43-35
   Show/Hide
C15H9FO2S
  1
1 IC50 = 461 nM
CP0572408
 Compound Info 
US8614253, 43-58
   Show/Hide
C15H11FO4
  1
1 IC50 = 471 nM
CP0419934
 Compound Info 
US8614253, 43-59
   Show/Hide
C14H9FO4
  1
1 IC50 = 495 nM
CP0117557
 Compound Info 
US8614253, 42-3
   Show/Hide
C11H7BrO2
  1
1 IC50 = 509 nM
CP0172113
 Compound Info 
US8614253, 26-27
   Show/Hide
C11H9N3O4
  1
1 IC50 = 535 nM
CP0557521
 Compound Info 
US8614253, 43-48
   Show/Hide
C15H12O5
  1
1 IC50 = 540 nM
CP0318244
 Compound Info 
US9241942, 38-10
   Show/Hide
C9H8BrN5O2
  1
1 IC50 = 587 nM
CP0117460
 Compound Info 
US8614253, 29-20
   Show/Hide
C18H12O4
  1
1 IC50 = 594 nM
CP0175328
 Compound Info 
US8614253, 43-75
   Show/Hide
C16H14FNO3
  1
1 IC50 = 633 nM
CP0123231
 Compound Info 
US8614253, 38-13
   Show/Hide
C11H9BrN2O2S
  1
1 IC50 = 641 nM
CP0132935
 Compound Info 
US8614253, 32-7
   Show/Hide
C21H18N2O4
  1
1 IC50 = 645 nM
CP0174196
 Compound Info 
US8614253, 43-78
   Show/Hide
C18H17NO4
  1
1 IC50 = 657 nM
CP0359891
 Compound Info 
US8614253, 43-17
   Show/Hide
C11H8O2S
  1
1 IC50 = 699 nM
CP0561453
 Compound Info 
US8614253, 43-33
   Show/Hide
C12H7F3O2S
  1
1 IC50 = 704 nM
CP0251333
 Compound Info 
US8614253, 3-31
   Show/Hide
C7H4Br2O2
  1
1 IC50 = 720 nM
CP0123223
 Compound Info 
US8614253, 43-52
   Show/Hide
C15H11NO6
  1
1 IC50 = 736 nM
CP0240985
 Compound Info 
US8614253, 26-7
   Show/Hide
C13H12O3S
  1
1 IC50 = 743 nM
CP0123215
 Compound Info 
US8614253, 26-23
   Show/Hide
C16H10N2O4
  1
1 IC50 = 754 nM
CP0215124
 Compound Info 
US8614253, 43-39
   Show/Hide
C19H19NO5
  1
1 IC50 = 795 nM
CP0117466
 Compound Info 
US9241942, 37-3
   Show/Hide
C14H10O3S
  1
1 IC50 = 799 nM
CP0187855
 Compound Info 
US8614253, 43-84
   Show/Hide
C12H7F3O3
  1
1 IC50 = 800 nM
CP0252055
 Compound Info 
US8614253, 26-20
   Show/Hide
C13H8F3NO2
  1
1 IC50 = 800 nM
CP0220215
 Compound Info 
US8614253, 29-17
   Show/Hide
C18H13NO3
  1
1 IC50 = 878 nM
CP0833545
 Compound Info 
US8614253, 35-2::US9241942, 35-2
   Show/Hide
C11H9NO3
  1
1 IC50 = 915 nM
CP0164710
 Compound Info 
US8614253, 26-11
   Show/Hide
C17H13NO3
  1
1 IC50 = 932 nM
CP0252054
 Compound Info 
US8614253, 26-18
   Show/Hide
C12H10FNO3
  1
1 IC50 = 994 nM
CP0121353
 Compound Info 
US8614253, 43-18
   Show/Hide
C12H11NO3
  1
1 IC50 = 1011 nM
CP0514850
 Compound Info 
4-amino-N-[6-chloro-3-[(2,5-difluorophenyl)sulfonylamino]-2-fluorophenyl]-6-methylquinazoline-8-carboxamide
   Show/Hide
C22H15ClF3N5O3S
  1
1 IC50 = 1100 nM
CP0246190
 Compound Info 
US8614253, 43-9
   Show/Hide
C13H13NO4
  1
1 IC50 = 1112 nM
CP0246192
 Compound Info 
US8614253, 43-44
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C18H16N2O6
  1
1 IC50 = 1202 nM
CP0359890
 Compound Info 
US8614253, 34-3
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C10H7NO2
  1
1 IC50 = 1240 nM
CP0187888
 Compound Info 
US8614253, 43-66
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C16H14N2O5
  1
1 IC50 = 1242 nM
CP0132934
 Compound Info 
US8614253, 32-1
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C23H21NO3
  1
1 IC50 = 1345 nM
CP0132835
 Compound Info 
US8614253, 38-4
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C28H28N2O4S4
  1
1 IC50 = 1348 nM
CP0324486
 Compound Info 
US9241942, 38-4
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C28H28N2O5S3
  1
1 IC50 = 1348 nM
CP0216837
 Compound Info 
US8614253, 43-15
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C16H12O3S
  1
1 IC50 = 1472 nM
CP0256673
 Compound Info 
4-amino-N-[6-chloro-3-[(2,5-difluorophenyl)sulfonylamino]-2-fluorophenyl]-6-pyridin-4-ylquinazoline-8-carboxamide
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C26H16ClF3N6O3S
  1
1 IC50 = 1600 nM
CP0370827
 Compound Info 
US8614253, 43-32
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C15H9FO2S
  1
1 IC50 = 1622 nM
CP0492248
 Compound Info 
4-amino-N-[6-chloro-3-[(2,5-difluorophenyl)sulfonylamino]-2-fluorophenyl]-6-(1-methylpyrazol-3-yl)quinazoline-8-carboxamide
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C25H17ClF3N7O3S
  1
1 IC50 = 1700 nM
CP0299939
 Compound Info 
US8614253, 43-54
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C15H14O5S
  1
1 IC50 = 1711 nM
CP0123220
 Compound Info 
US8614253, 43-20
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C15H12O3
  1
1 IC50 = 1797 nM
CP0578280
 Compound Info 
4-amino-N-[6-chloro-3-[(2,5-difluorophenyl)sulfonylamino]-2-fluorophenyl]-6-(2-methylpyrazol-3-yl)quinazoline-8-carboxamide
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C25H17ClF3N7O3S
  1
1 IC50 = 2000 nM
CP0353146
 Compound Info 
US8614253, 29-8
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C18H14O3
  1
1 IC50 = 2016 nM
CP0172034
 Compound Info 
US8614253, 38-1
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C20H22Br2N2O4S2
  1
1 IC50 = 2117 nM
CP0137278
 Compound Info 
US8614253, 26-16
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C15H9NO4S
  1
1 IC50 = 2369 nM
CP0412227
 Compound Info 
US8614253, 43-45
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C14H11NO6S
  1
1 IC50 = 2795 nM
CP0358898
 Compound Info 
US8614253, 32-3
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C26H21NO3
  2
1 IC50 = 2806 nM
2 IC50 = 2808 nM
CP0960214
 Compound Info 
US9241942, 27-19
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C13H12N2O4
  1
1 IC50 = 3059 nM
CP0568516
 Compound Info 
4-amino-N-[6-chloro-3-[(2,5-difluorophenyl)sulfonylamino]-2-fluorophenyl]-6-(1H-pyrazol-4-yl)quinazoline-8-carboxamide
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C24H15ClF3N7O3S
  1
1 IC50 = 3200 nM
CP0479228
 Compound Info 
US8614253, 43-50
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C17H16O5
  1
1 IC50 = 3309 nM
CP0292674
 Compound Info 
US8614253, 43-49
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C17H14F3NO3
  1
1 IC50 = 3670 nM
CP0117462
 Compound Info 
US8614253, 32-5
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C26H21NO3
  1
1 IC50 = 3797 nM
CP0172114
 Compound Info 
US8614253, 43-14
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C16H12O3S
  1
1 IC50 = 3906 nM
CP0516235
 Compound Info 
US8614253, 36-3
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C10H12BrNO2S
  1
1 IC50 = 4146 nM
CP0358896
 Compound Info 
US8614253, 29-7
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C15H10O3
  1
1 IC50 = 4202 nM
CP0117441
 Compound Info 
US8614253, 43-24
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C15H10O2S
  1
1 IC50 = 4503 nM
CP0252058
 Compound Info 
US8614253, 43-53
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C15H12O5
  1
1 IC50 = 4784 nM
CP0362665
 Compound Info 
4-amino-N-[6-chloro-3-[(2,5-difluorophenyl)sulfonylamino]-2-fluorophenyl]-6-pyridin-3-ylquinazoline-8-carboxamide
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C26H16ClF3N6O3S
  1
1 IC50 = 4900 nM
CP0553172
 Compound Info 
4-amino-N-[6-chloro-3-[(2,5-difluorophenyl)sulfonylamino]-2-fluorophenyl]thieno[3,2-d]pyrimidine-7-carboxamide
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C19H11ClF3N5O3S2
  1
1 IC50 = 5300 nM
CP0545824
 Compound Info 
4-amino-N-[6-chloro-2-fluoro-3-(pyrrolidin-1-ylsulfonylamino)phenyl]quinazoline-8-carboxamide
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C19H18ClFN6O3S
  1
1 IC50 = 5580 nM
CP0346880
 Compound Info 
US8614253, 29-1
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C19H14O4
  1
1 IC50 = 5665 nM
CP0325733
 Compound Info 
US8614253, 29-12
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C20H13NO2
  1
1 IC50 = 6277 nM
CP0121352
 Compound Info 
US8614253, 43-3
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C16H14O5
  1
1 IC50 = 7344 nM
CP0117457
 Compound Info 
US8614253, 29-9
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C17H13NO3
  1
1 IC50 = 8737 nM
CP0114463
 Compound Info 
US8614253, 36-1
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C11H12BrNO4S
  1
1 IC50 = 8796 nM
CP0563849
 Compound Info 
US8614253, 29-10
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C15H10O2S
  1
1 IC50 = 9371 nM
CP0567600
 Compound Info 
N-[6-chloro-3-[(2,5-difluorophenyl)sulfonylamino]-2-fluorophenyl]-6-methyl-4-[[(3S)-piperidin-3-yl]amino]quinazoline-8-carboxamide
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C27H24ClF3N6O3S
  1
1 IC50 = 9900 nM
CP0328536
 Compound Info 
US8614253, 39-2
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C17H19NO2
  1
1 IC50 = 11375 nM
CP0117458
 Compound Info 
US8614253, 29-11
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C20H13NO2
  1
1 IC50 = 12122 nM
CP0553171
 Compound Info 
4-amino-N-[6-chloro-3-[(2,5-difluorophenyl)sulfonylamino]-2-fluorophenyl]quinazoline-8-carboxamide
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C21H13ClF3N5O3S
  1
1 IC50 = 12700 nM
CP0173582
 Compound Info 
US8614253, 36-2
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C13H16BrNO4S
  1
1 IC50 = 17662 nM
CP0267608
 Compound Info 
CHEMBL4753081
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C28H27Cl2F3N6O3S
  1
1 IC50 = 19000 nM
CP0514851
 Compound Info 
N-[6-chloro-3-[(2,5-difluorophenyl)sulfonylamino]-2-fluorophenyl]-6-methyl-4-[[(3R)-piperidin-3-yl]amino]quinazoline-8-carboxamide
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C27H24ClF3N6O3S
  1
1 IC50 = 19000 nM
CP0331095
 Compound Info 
US8614253, 43-70
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C12H10N2O3
  1
1 IC50 = 20111 nM
CP0492249
 Compound Info 
N-[6-chloro-3-[(2,5-difluorophenyl)sulfonylamino]-2-fluorophenyl]-4-[2-(dimethylamino)ethylamino]-6-methylquinazoline-8-carboxamide
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C26H24ClF3N6O3S
  1
1 IC50 = 29000 nM
CP0568502
 Compound Info 
4-(2-aminoethylamino)-N-[6-chloro-3-[(2,5-difluorophenyl)sulfonylamino]-2-fluorophenyl]-6-methylquinazoline-8-carboxamide
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C24H20ClF3N6O3S
  1
1 IC50 = 31000 nM
CP0349117
 Compound Info 
US8614253, 42-11
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C11H9NO2
  1
1 IC50 = 36370 nM
CP0107278
 Compound Info 
US8614253, 29-15
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C18H13ClO2
  1
1 IC50 > 20000 nM
CP0114753
 Compound Info 
US8614253, 36-6
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C11H10BrNO5S
  1
1 IC50 > 20000 nM
CP0117440
 Compound Info 
US8614253, 43-23
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C15H10O2S
  2
1 IC50 < 20000 nM
2 IC50 > 20000 nM
CP0117464
 Compound Info 
US8614253, 36-8
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C14H15NO2S2
  1
1 IC50 > 20000 nM
CP0216819
 Compound Info 
US8614253, 29-14
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C18H13ClO2
  1
1 IC50 > 20000 nM
CP0252090
 Compound Info 
US8614253, 29-21
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C20H18N2O3
  1
1 IC50 > 20000 nM
CP0259855
 Compound Info 
US8614253, 26-3
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C12H8N2O4
  1
1 IC50 > 20000 nM
CP0259872
 Compound Info 
US8614253, 38-15
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C17H14N2O2S
  1
1 IC50 > 20000 nM
CP0325734
 Compound Info 
US8614253, 29-13
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C18H13FO2
  1
1 IC50 > 20000 nM
CP0325737
 Compound Info 
US8614253, 36-10
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C12H13Br2NO4S
  1
1 IC50 > 20000 nM
CP0331107
 Compound Info 
US8614253, 36-9
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C15H15NO4S2
  1
1 IC50 > 20000 nM
CP0348262
 Compound Info 
US8614253, 36-5
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C10H10BrNO3S
  1
1 IC50 > 20000 nM
CP0518990
 Compound Info 
US8614253, 36-7
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C14H17Br2NO4S
  1
1 IC50 > 20000 nM
CP0202750
 Compound Info 
8-hydroxy-3-methyl-5-oxo-2,4-dihydro-1H-chromeno[3,4-c]pyridine-7-carbaldehyde
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C14H13NO4
  1
1 Kd = 138 nM
Clinical Information about the Protein
Target 1 ( Endoplasmic reticulum to nucleus signaling 1 (ERN1) )
Target Type Clinical trial Target
Target 2 ( Inositol-requiring protein 1 (IRE1a) )
Target Type Literature-reported Target