Reaction Details
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Signal transducer and activator of transcription 1-alpha/beta
Ligand
BDBM50514302
Substrate
n/a
Meas. Tech.
ChEMBL_1856063 (CHEMBL4356792)
Kd
1000±n/a nM
Citation
Zhou, H; Bai, L; Xu, R; Zhao, Y; Chen, J; McEachern, D; Chinnaswamy, K; Wen, B; Dai, L; Kumar, P; Yang, CY; Liu, Z; Wang, M; Liu, L; Meagher, JL; Yi, H; Sun, D; Stuckey, JA; Wang, S Structure-Based Discovery of SD-36 as a Potent, Selective, and Efficacious PROTAC Degrader of STAT3 Protein. J Med Chem 62:11280-11300 (2019) [PubMed] Article More Info.:
Target
Name:
Signal transducer and activator of transcription 1-alpha/beta
Synonyms:
Signal transducer and activator of transcription 1-alpha/beta | Transcription factor ISGF-3 components p91/p84 | signal transducer and activator of transcription 1 isoform alpha | STAT1_HUMAN | STAT1 | Transcription Factor STAT1
Type:
Cytosolic Transcription Factor
Mol. Mass.:
87327.69
Organism:
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:
BDBM50514302
Synonyms:
CHEMBL4452527
Type:
Small organic molecule
Emp. Form.:
C59H62F2N9O12P
Mol. Mass.:
1158.17
SMILES:
[H][C@]12CC[C@H](N1C(=O)[C@H](CN(CC2)C(=O)CCCCCC#Cc1cccc2C(=O)N(Cc12)C1CCC(=O)NC1=O)NC(=O)c1cc2cc(ccc2[nH]1)C(F)(F)P(O)(O)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(c1ccccc1)c1ccccc1 |r|
