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Assay Detail

CHEMBL5111285

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human recombinant STAT3 (127 to 722 residues) transcriptional activity expressed in HEK293T cells in presence of IL-6 by Dual-luciferase reporter gene assay
56
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Signal transducer and activator of transcription 3 (CHEMBL4026)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Novel Potent STAT3 Inhibitor HP590 with Dual p-Tyr<sup>705</sup>/Ser<sup>727</sup> Inhibitory Activity for Gastric Cancer Treatment.
He P, Miao Y, Sun Y, Bian A, Jin W, Chen H, Ye J, He J, Peng Y, Gu H, Liu M, Yi Z, Chen Y.
J Med Chem (2022) 65 : 12650 -12674
PubMed 36103247 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 56 6.81 7.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5176684 1 7.56
CHEMBL5176948 1 7.49
CHEMBL5182844 1 7.43
CHEMBL5199234 1 7.40
CHEMBL5185530 1 7.40
CHEMBL5196490 1 7.28
CHEMBL5189947 1 7.24
CHEMBL5170615 1 7.22
CHEMBL5182625 1 7.20
CHEMBL5171708 1 7.12
CHEMBL5177332 1 7.05
CHEMBL5189774 1 7.03
CHEMBL5183263 1 7.03
CHEMBL5199713 1 6.96
CHEMBL5200334 1 6.95
CHEMBL5189465 1 6.95
CHEMBL5189640 1 6.91
CHEMBL5204997 1 6.89
CHEMBL5175537 1 6.83
CHEMBL5182268 1 6.78
CHEMBL5196843 1 6.76
CHEMBL5199802 1 6.75
CHEMBL5191059 1 6.74
CHEMBL5204672 1 6.59
CHEMBL5190384 1 6.57
CHEMBL5189435 1 6.56
CHEMBL5208052 1 6.53
CHEMBL5199392 1 6.52
CHEMBL5191928 1 6.51
CHEMBL5205208 1 6.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5176684 IC50 = 27.8 nM 7.56
CHEMBL5176948 IC50 = 32.3 nM 7.49
CHEMBL5182844 IC50 = 37.4 nM 7.43
CHEMBL5199234 IC50 = 40.2 nM 7.40
CHEMBL5185530 IC50 = 40.2 nM 7.40
CHEMBL5196490 IC50 = 52.1 nM 7.28
CHEMBL5189947 IC50 = 58.0 nM 7.24
CHEMBL5170615 IC50 = 60.2 nM 7.22
CHEMBL5182625 IC50 = 63.6 nM 7.20
CHEMBL5171708 IC50 = 75.9 nM 7.12
CHEMBL5177332 IC50 = 88.1 nM 7.05
CHEMBL5189774 IC50 = 93.2 nM 7.03
CHEMBL5183263 IC50 = 94.1 nM 7.03
CHEMBL5199713 IC50 = 108.5 nM 6.96
CHEMBL5189465 IC50 = 113.3 nM 6.95
CHEMBL5200334 IC50 = 112.7 nM 6.95
CHEMBL5189640 IC50 = 123.3 nM 6.91
CHEMBL5204997 IC50 = 129.7 nM 6.89
CHEMBL5175537 IC50 = 147.5 nM 6.83
CHEMBL5182268 IC50 = 167.3 nM 6.78
CHEMBL5196843 IC50 = 172.7 nM 6.76
CHEMBL5199802 IC50 = 177.4 nM 6.75
CHEMBL5191059 IC50 = 181.9 nM 6.74
CHEMBL5204672 IC50 = 257.5 nM 6.59
CHEMBL5190384 IC50 = 270.5 nM 6.57
CHEMBL5189435 IC50 = 272.9 nM 6.56
CHEMBL5208052 IC50 = 295.7 nM 6.53
CHEMBL5199392 IC50 = 304.0 nM 6.52
CHEMBL5191928 IC50 = 305.6 nM 6.51
CHEMBL5205208 IC50 = 325.4 nM 6.49
CHEMBL5208462 IC50 = 358.9 nM 6.45
CHEMBL5189395 IC50 = 476.9 nM 6.32
CHEMBL5175861 IC50 = 515.7 nM 6.29
CHEMBL5191288 IC50 = 533.2 nM 6.27
CHEMBL5186501 IC50 = 564.0 nM 6.25
CHEMBL5207761 IC50 = 802.5 nM 6.10
CHEMBL5186045 IC50 = 2792.1 nM 5.55
CHEMBL5177779 IC50 > 1000.0 nM -
CHEMBL5202700 IC50 > 1000.0 nM -
CHEMBL5189463 IC50 > 1000.0 nM -
CHEMBL5202773 IC50 > 1000.0 nM -
CHEMBL5178453 IC50 > 1000.0 nM -
CHEMBL5203423 IC50 > 1000.0 nM -
CHEMBL5184061 IC50 > 1000.0 nM -
CHEMBL5189078 IC50 > 1000.0 nM -
CHEMBL5169556 IC50 > 1000.0 nM -
CHEMBL5193929 IC50 > 1000.0 nM -
CHEMBL5203071 IC50 > 1000.0 nM -
CHEMBL5189121 IC50 > 1000.0 nM -
CHEMBL64130 NAPABUCASIN IC50 - -