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Assay Detail

CHEMBL2214835

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

Binding
Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins prior to IL6-induction measured after 30 to 45 mins
ChEMBL ↗
38
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type TF-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2.
Labadie S, Dragovich PS, Barrett K, Blair WS, Bergeron P, Chang C, Deshmukh G, Eigenbrot C, Ghilardi N, Gibbons P, Hurley CA, Johnson A, Kenny JR, Kohli PB, Kulagowski JJ, Liimatta M, Lupardus PJ, Mendonca R, Murray JM, Pulk R, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward S, Zak M.
Bioorg Med Chem Lett (2012) 22 : 7627 -7633
PubMed 23107482 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 38 6.36 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2206059 — — 1 7.89
CHEMBL2206638 — — 2 7.52
CHEMBL2152401 — — 1 7.37
CHEMBL2206639 — — 1 7.30
CHEMBL2206629 — — 2 7.07
CHEMBL2206636 — — 1 6.89
CHEMBL2206637 — — 1 6.80
CHEMBL2206058 — — 1 6.80
CHEMBL2206061 — — 1 6.80
CHEMBL2206634 — — 1 6.75
CHEMBL2206633 — — 1 6.72
CHEMBL2206632 — — 1 6.68
CHEMBL2206060 — — 1 6.56
CHEMBL2206626 — — 1 6.49
CHEMBL2206062 — — 1 6.39
CHEMBL2206611 — — 1 6.37
CHEMBL2206614 — — 1 6.24
CHEMBL2206620 — — 1 6.20
CHEMBL2206631 — — 1 6.17
CHEMBL2206635 — — 1 6.09
CHEMBL2206622 — — 1 5.92
CHEMBL2206613 — — 1 5.89
CHEMBL2206627 — — 2 5.89
CHEMBL2206625 — — 1 5.82
CHEMBL2206617 — — 1 5.75
CHEMBL2206612 — — 1 5.70
CHEMBL2206628 — — 1 5.66
CHEMBL2206618 — — 1 5.58
CHEMBL2206615 — — 1 5.58
CHEMBL2206630 — — 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2206059 — EC50 = 13.0 nM 7.89
CHEMBL2206638 — EC50 = 30.0 nM 7.52
CHEMBL2152401 — EC50 = 43.0 nM 7.37
CHEMBL2206639 — EC50 = 50.0 nM 7.30
CHEMBL2206629 — EC50 = 86.0 nM 7.07
CHEMBL2206636 — EC50 = 130.0 nM 6.89
CHEMBL2206637 — EC50 = 160.0 nM 6.80
CHEMBL2206058 — EC50 = 160.0 nM 6.80
CHEMBL2206061 — EC50 = 160.0 nM 6.80
CHEMBL2206634 — EC50 = 180.0 nM 6.75
CHEMBL2206633 — EC50 = 190.0 nM 6.72
CHEMBL2206632 — EC50 = 210.0 nM 6.68
CHEMBL2206060 — EC50 = 275.0 nM 6.56
CHEMBL2206626 — EC50 = 325.0 nM 6.49
CHEMBL2206638 — EC50 = 355.0 nM 6.45
CHEMBL2206062 — EC50 = 410.0 nM 6.39
CHEMBL2206611 — EC50 = 430.0 nM 6.37
CHEMBL2206614 — EC50 = 570.0 nM 6.24
CHEMBL2206620 — EC50 = 625.0 nM 6.20
CHEMBL2206631 — EC50 = 670.0 nM 6.17
CHEMBL2206635 — EC50 = 815.0 nM 6.09
CHEMBL2206622 — EC50 = 1200.0 nM 5.92
CHEMBL2206627 — EC50 = 1300.0 nM 5.89
CHEMBL2206613 — EC50 = 1300.0 nM 5.89
CHEMBL2206625 — EC50 = 1500.0 nM 5.82
CHEMBL2206629 — EC50 = 1600.0 nM 5.80
CHEMBL2206617 — EC50 = 1800.0 nM 5.75
CHEMBL2206612 — EC50 = 2000.0 nM 5.70
CHEMBL2206628 — EC50 = 2200.0 nM 5.66
CHEMBL2206618 — EC50 = 2600.0 nM 5.58
CHEMBL2206615 — EC50 = 2600.0 nM 5.58
CHEMBL2206630 — EC50 = 4200.0 nM 5.38
CHEMBL2206616 — EC50 = 5200.0 nM 5.28
CHEMBL2206619 — EC50 > 3800.0 nM -
CHEMBL2206621 — EC50 > 3500.0 nM -
CHEMBL2206623 — EC50 > 6500.0 nM -
CHEMBL2206624 — EC50 > 6000.0 nM -
CHEMBL2206627 — EC50 > 5300.0 nM -