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Target
Signal transducer and activator of transcription 1-alpha/beta
Ligand
BDBM50190100
Substrate
n/a
Meas. Tech.
Bioassay Evaluation
IC50
>50000±n/a nM
Citation
 Huryn, DM; Wipf, P; Grandis, JR; LaPorte, MG; Johnston, PA; Schurdak, ME; Colombo, R 6-aryl-7-substituted-3-(1H-pyrazol-5-yl)-7H-[1,2,4]triazolo[3,4-B][1,3,4]thiadiazines as inhibitors of the STAT3 pathway with anti-proliferative activity US Patent  US10618914 Publication Date 4/14/2020 
Target
Name:
Signal transducer and activator of transcription 1-alpha/beta
Synonyms:
STAT1 | STAT1_HUMAN | Signal transducer and activator of transcription 1-alpha/beta | Transcription Factor STAT1 | Transcription factor ISGF-3 components p91/p84 | signal transducer and activator of transcription 1 isoform alpha
Type:
Cytosolic Transcription Factor
Mol. Mass.:
87327.69
Organism:
Homo sapiens (Human)
Description:
Stat1 was expressed in sf9 cells from a baculovirus encoding the recombinant proteins. Stat1 dimer binds to DNA.
Residue:
750
Sequence:
MSQWYELQQLDSKFLEQVHQLYDDSFPMEIRQYLAQWLEKQDWEHAANDVSFATIRFHDLLSQLDDQYSRFSLENNFLLQHNIRKSKRNLQDNFQEDPIQMSMIIYSCLKEERKILENAQRFNQAQSGNIQSTVMLDKQKELDSKVRNVKDKVMCIEHEIKSLEDLQDEYDFKCKTLQNREHETNGVAKSDQKQEQLLLKKMYLMLDNKRKEVVHKIIELLNVTELTQNALINDELVEWKRRQQSACIGGPPNACLDQLQNWFTIVAESLQQVRQQLKKLEELEQKYTYEHDPITKNKQVLWDRTFSLFQQLIQSSFVVERQPCMPTHPQRPLVLKTGVQFTVKLRLLVKLQELNYNLKVKVLFDKDVNERNTVKGFRKFNILGTHTKVMNMEESTNGSLAAEFRHLQLKEQKNAGTRTNEGPLIVTEELHSLSFETQLCQPGLVIDLETTSLPVVVISNVSQLPSGWASILWYNMLVAEPRNLSFFLTPPCARWAQLSEVLSWQFSSVTKRGLNVDQLNMLGEKLLGPNASPDGLIPWTRFCKENINDKNFPFWLWIESILELIKKHLLPLWNDGCIMGFISKERERALLKDQQPGTFLLRFSESSREGAITFTWVERSQNGGEPDFHAVEPYTKKELSAVTFPDIIRNYKVMAAENIPENPLKYLYPNIDKDHAFGKYYSRPKEAPEPMELDGPKGTGYIKTELISVSEVHPSRLQTTDNLLPMSPEEFDEVSRIVGSVEFDSMMNTV
  
Inhibitor
Name:
BDBM50190100
Synonyms:
CHEMBL3827123 | US10618914, Compound 26 | US11111253, Compound 26
Type:
Small organic molecule
Emp. Form.:
C20H22N6OS
Mol. Mass.:
394.493
SMILES:
COc1ccc(cc1)C1=Nn2c(SC1C(C)C)nnc2-c1[nH]nc2CCCc12 |t:9|
Structure:
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