Reaction Details |
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Target | Signal transducer and activator of transcription 1-alpha/beta |
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Ligand | BDBM50189922 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1591093 (CHEMBL3829061) |
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IC50 | >50000±n/a nM |
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Citation | LaPorte, MG; Wang, Z; Colombo, R; Garzan, A; Peshkov, VA; Liang, M; Johnston, PA; Schurdak, ME; Sen, M; Camarco, DP; Hua, Y; Pollock, NI; Lazo, JS; Grandis, JR; Wipf, P; Huryn, DM Optimization of pyrazole-containing 1,2,4-triazolo-[3,4-b]thiadiazines, a new class of STAT3 pathway inhibitors. Bioorg Med Chem Lett26:3581-5 (2016) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Signal transducer and activator of transcription 1-alpha/beta |
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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: | MSQWYELQQLDSKFLEQVHQLYDDSFPMEIRQYLAQWLEKQDWEHAANDVSFATIRFHDL
LSQLDDQYSRFSLENNFLLQHNIRKSKRNLQDNFQEDPIQMSMIIYSCLKEERKILENAQ
RFNQAQSGNIQSTVMLDKQKELDSKVRNVKDKVMCIEHEIKSLEDLQDEYDFKCKTLQNR
EHETNGVAKSDQKQEQLLLKKMYLMLDNKRKEVVHKIIELLNVTELTQNALINDELVEWK
RRQQSACIGGPPNACLDQLQNWFTIVAESLQQVRQQLKKLEELEQKYTYEHDPITKNKQV
LWDRTFSLFQQLIQSSFVVERQPCMPTHPQRPLVLKTGVQFTVKLRLLVKLQELNYNLKV
KVLFDKDVNERNTVKGFRKFNILGTHTKVMNMEESTNGSLAAEFRHLQLKEQKNAGTRTN
EGPLIVTEELHSLSFETQLCQPGLVIDLETTSLPVVVISNVSQLPSGWASILWYNMLVAE
PRNLSFFLTPPCARWAQLSEVLSWQFSSVTKRGLNVDQLNMLGEKLLGPNASPDGLIPWT
RFCKENINDKNFPFWLWIESILELIKKHLLPLWNDGCIMGFISKERERALLKDQQPGTFL
LRFSESSREGAITFTWVERSQNGGEPDFHAVEPYTKKELSAVTFPDIIRNYKVMAAENIP
ENPLKYLYPNIDKDHAFGKYYSRPKEAPEPMELDGPKGTGYIKTELISVSEVHPSRLQTT
DNLLPMSPEEFDEVSRIVGSVEFDSMMNTV
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BDBM50189922 |
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n/a |
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Name | BDBM50189922 |
Synonyms: | CHEMBL1527817 | US10618914, Compound 1a | US11111253, Compound 1a |
Type | Small organic molecule |
Emp. Form. | C16H12Cl2N6S |
Mol. Mass. | 391.278 |
SMILES | Clc1ccc(cc1Cl)C1=Nn2c(SC1)nnc2-c1[nH]nc2CCCc12 |t:9| |
Structure |
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