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Assay Detail

CHEMBL3388143

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

Binding
Inhibition of human recombinant JAK1
ChEMBL ↗
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tyrosine-protein kinase JAK1 (CHEMBL2835) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.
Menet CJ, Fletcher SR, Van Lommen G, Geney R, Blanc J, Smits K, Jouannigot N, Deprez P, van der Aar EM, Clement-Lacroix P, Lepescheux L, Galien R, Vayssiere B, Nelles L, Christophe T, Brys R, Uhring M, Ciesielski F, Van Rompaey L.
J Med Chem (2014) 57 : 9323 -9342
PubMed 25369270 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 6.98 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3360349 — — 1 9.22
CHEMBL221959 TOFACITINIB 4.0 1 9.10
CHEMBL1789941 RUXOLITINIB 4.0 1 8.92
CHEMBL3360351 — — 1 8.85
CHEMBL3360330 — — 1 8.55
CHEMBL3360350 — — 1 8.08
CHEMBL3301607 FILGOTINIB 4.0 1 8.00
CHEMBL3360355 — — 1 7.80
CHEMBL3360348 — — 1 7.64
CHEMBL3360356 — — 1 7.57
CHEMBL3360341 — — 1 7.57
CHEMBL3360357 — — 1 7.39
CHEMBL3360343 — — 1 7.17
CHEMBL3360318 — — 1 7.16
CHEMBL3360353 — — 1 7.04
CHEMBL3360339 — — 1 6.99
CHEMBL2414557 — — 1 6.85
CHEMBL3360352 — — 1 6.83
CHEMBL2414558 — — 1 6.81
CHEMBL3360332 — — 1 6.74
CHEMBL3360840 — — 1 6.51
CHEMBL3360333 — — 1 6.43
CHEMBL3360328 — — 1 6.38
CHEMBL3360344 — — 1 6.38
CHEMBL3360335 — — 1 6.26
CHEMBL3360338 — — 1 6.24
CHEMBL3360336 — — 1 6.01
CHEMBL3360337 — — 1 5.87
CHEMBL3360331 — — 1 5.70
CHEMBL3360334 — — 1 5.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3360349 — IC50 = 0.6 nM 9.22
CHEMBL221959 TOFACITINIB IC50 = 0.8 nM 9.10
CHEMBL1789941 RUXOLITINIB IC50 = 1.2 nM 8.92
CHEMBL3360351 — IC50 = 1.4 nM 8.85
CHEMBL3360330 — IC50 = 2.8 nM 8.55
CHEMBL3360350 — IC50 = 8.3 nM 8.08
CHEMBL3301607 FILGOTINIB IC50 = 10.0 nM 8.00
CHEMBL3360355 — IC50 = 16.0 nM 7.80
CHEMBL3360348 — IC50 = 23.0 nM 7.64
CHEMBL3360356 — IC50 = 27.0 nM 7.57
CHEMBL3360341 — IC50 = 27.0 nM 7.57
CHEMBL3360357 — IC50 = 41.0 nM 7.39
CHEMBL3360343 — IC50 = 67.0 nM 7.17
CHEMBL3360318 — IC50 = 70.0 nM 7.16
CHEMBL3360353 — IC50 = 92.0 nM 7.04
CHEMBL3360339 — IC50 = 103.0 nM 6.99
CHEMBL2414557 — IC50 = 142.0 nM 6.85
CHEMBL3360352 — IC50 = 147.0 nM 6.83
CHEMBL2414558 — IC50 = 156.0 nM 6.81
CHEMBL3360332 — IC50 = 184.0 nM 6.74
CHEMBL3360840 — IC50 = 307.0 nM 6.51
CHEMBL3360333 — IC50 = 371.0 nM 6.43
CHEMBL3360344 — IC50 = 418.0 nM 6.38
CHEMBL3360328 — IC50 = 413.0 nM 6.38
CHEMBL3360335 — IC50 = 547.0 nM 6.26
CHEMBL3360338 — IC50 = 572.0 nM 6.24
CHEMBL3360336 — IC50 = 975.0 nM 6.01
CHEMBL3360337 — IC50 = 1351.0 nM 5.87
CHEMBL3360331 — IC50 = 1979.0 nM 5.70
CHEMBL3360334 — IC50 = 2554.0 nM 5.59
CHEMBL3360342 — IC50 = 3012.0 nM 5.52
CHEMBL3360319 — IC50 = 3055.0 nM 5.51
CHEMBL3360347 — IC50 = 3098.0 nM 5.51
CHEMBL3352896 — IC50 = 5740.0 nM 5.24
CHEMBL3360340 — IC50 > 10000.0 nM -
CHEMBL3360320 — IC50 > 10000.0 nM -
CHEMBL3360321 — IC50 > 10000.0 nM -
CHEMBL3360322 — IC50 > 10000.0 nM -
CHEMBL3360354 — IC50 > 4000.0 nM -
CHEMBL3360323 — IC50 > 10000.0 nM -
CHEMBL3360324 — IC50 > 4000.0 nM -
CHEMBL3360325 — IC50 > 10000.0 nM -
CHEMBL3360326 — IC50 > 10000.0 nM -
CHEMBL3360327 — IC50 > 10000.0 nM -
CHEMBL3360329 — IC50 > 10000.0 nM -
CHEMBL3360345 — IC50 - — -
CHEMBL3360346 — IC50 - — -