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Assay Detail

CHEMBL5375116

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

Binding
Inhibition of JAK1/2-mediated STAT1 phosphorylation in human M07E cells preincubated for 30 mins followed by IFN-alpha stimulation measured after 15 mins by flow cytometry
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type M07E
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

JAK2/JAK1 (CHEMBL3038492)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Design of a Supersoft Topical JAK Inhibitor, Which Is Effective in Human Skin but Rapidly Deactivated in Blood.
Thoma G, Decoret O, Vangrevelinghe E, Trunzer M, Decker A, Orjuela Leon A, Beerli C, Bruno S, Hauchard A, Paulat G, Zerwes HG, Hacini-Rachinel F.
J Med Chem (2023) 66 : 15042 -15053
PubMed 37906573 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.04 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5422886 1 7.85
CHEMBL5409953 1 7.43
CHEMBL5396554 1 7.36
CHEMBL5404574 1 7.35
CHEMBL5407260 1 7.32
CHEMBL5412967 1 7.24
CHEMBL5420083 1 7.24
CHEMBL5403897 1 7.22
CHEMBL5279787 1 7.15
CHEMBL5270549 1 7.07
CHEMBL5424439 1 6.94
CHEMBL5395839 1 6.73
CHEMBL5417474 1 6.73
CHEMBL5420971 1 6.54
CHEMBL5431257 1 5.41
CHEMBL5407329 1 -
CHEMBL5271559 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5422886 IC50 = 14.0 nM 7.85
CHEMBL5409953 IC50 = 37.0 nM 7.43
CHEMBL5396554 IC50 = 44.0 nM 7.36
CHEMBL5404574 IC50 = 45.0 nM 7.35
CHEMBL5407260 IC50 = 48.0 nM 7.32
CHEMBL5412967 IC50 = 58.0 nM 7.24
CHEMBL5420083 IC50 = 58.0 nM 7.24
CHEMBL5403897 IC50 = 60.0 nM 7.22
CHEMBL5279787 IC50 = 71.0 nM 7.15
CHEMBL5270549 IC50 = 85.0 nM 7.07
CHEMBL5424439 IC50 = 115.0 nM 6.94
CHEMBL5395839 IC50 = 185.0 nM 6.73
CHEMBL5417474 IC50 = 185.0 nM 6.73
CHEMBL5420971 IC50 = 288.0 nM 6.54
CHEMBL5431257 IC50 = 3861.0 nM 5.41
CHEMBL5407329 IC50 > 10000.0 nM -
CHEMBL5271559 IC50 > 10000.0 nM -