View interactive charts of activity data from GtoPdb and ChEMBL (where available) across species
Bioactivity Comments |
PF-06651600 exhibits favourable selectivity against a screening panel of 305 kinases in vitro, and shows measurable inhibition of 7 of the 10 other kinases which share a cysteine residue analogous to Cys-909 in the JAK3 ATP binding site (these were BMX, ITK, TXK, TEC, BTK, BLK and HER4) [3]. ATP concentration for JAK3 is 4 μM at Km and for JAK1 is 40 μM at Km, but some assays reported in [3] were carried out at 1 mM ATP . |
Selectivity at enzymes |
Key to terms and symbols
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Janus kinase 3
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Hs |
Inhibitor |
Inhibition |
9.5 |
pIC50 |
- |
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⤷ |
pIC50
9.5
(IC50 3x10-10 M)
Description: At 4 μM ATP (Km).
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Janus kinase 1
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Hs |
Inhibitor |
Inhibition |
5.8 |
pIC50 |
- |
3 |
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⤷ |
pIC50
5.8
(IC50 1.64x10-6 M)
[3]
Description: At 1 mM ATP.
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