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Assay Detail

CHEMBL4258465

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ADMET
Inhibition of human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate after 40 mins in presence of [gamma-33P-ATP] by scintillation counting method
ChEMBL ↗
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tyrosine-protein kinase JAK2 (CHEMBL2971) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and evaluation of (<i>R</i>)-3-(7-(methyl(7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidin-4-yl)amino)-5-azaspiro[2.4]heptan-5-yl)-3-oxopropanenitrile as a JAK1-selective inhibitor.
Chough C, Lee S, Joung M, Lee J, Kim JH, Kim BM.
Medchemcomm (2018) 9 : 477 -489
PubMed 30108938 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 6.07 8.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4279526 — — 1 8.26
CHEMBL4289789 — — 1 8.08
CHEMBL3301607 FILGOTINIB 4.0 1 7.55
CHEMBL4276966 — — 1 7.52
CHEMBL4285473 — — 1 7.44
CHEMBL4278452 — — 1 7.30
CHEMBL4283883 — — 1 7.29
CHEMBL4293578 — — 1 7.23
CHEMBL4284912 — — 1 7.18
CHEMBL4281921 — — 1 7.01
CHEMBL4291829 — — 1 6.89
CHEMBL4279402 — — 1 6.82
CHEMBL4287327 — — 1 6.82
CHEMBL4284136 — — 1 6.80
CHEMBL4283964 — — 1 6.75
CHEMBL4283965 — — 1 6.75
CHEMBL4292871 — — 1 6.60
CHEMBL4277098 — — 1 6.58
CHEMBL4279819 — — 1 6.39
CHEMBL4290931 — — 1 6.38
CHEMBL4290189 — — 1 6.33
CHEMBL4286370 — — 1 6.32
CHEMBL4295175 — — 1 6.03
CHEMBL4293482 — — 1 6.00
CHEMBL4282998 — — 1 5.96
CHEMBL4285014 — — 1 5.96
CHEMBL4276863 — — 1 5.92
CHEMBL4288323 — — 1 5.92
CHEMBL4285042 — — 1 5.89
CHEMBL4277099 — — 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4279526 — IC50 = 5.5 nM 8.26
CHEMBL4289789 — IC50 = 8.4 nM 8.08
CHEMBL3301607 FILGOTINIB IC50 = 28.0 nM 7.55
CHEMBL4276966 — IC50 = 30.0 nM 7.52
CHEMBL4285473 — IC50 = 36.0 nM 7.44
CHEMBL4278452 — IC50 = 50.0 nM 7.30
CHEMBL4283883 — IC50 = 51.0 nM 7.29
CHEMBL4293578 — IC50 = 59.0 nM 7.23
CHEMBL4284912 — IC50 = 66.0 nM 7.18
CHEMBL4281921 — IC50 = 97.0 nM 7.01
CHEMBL4291829 — IC50 = 130.0 nM 6.89
CHEMBL4279402 — IC50 = 150.0 nM 6.82
CHEMBL4287327 — IC50 = 150.0 nM 6.82
CHEMBL4284136 — IC50 = 160.0 nM 6.80
CHEMBL4283965 — IC50 = 180.0 nM 6.75
CHEMBL4283964 — IC50 = 180.0 nM 6.75
CHEMBL4292871 — IC50 = 250.0 nM 6.60
CHEMBL4277098 — IC50 = 260.0 nM 6.58
CHEMBL4279819 — IC50 = 410.0 nM 6.39
CHEMBL4290931 — IC50 = 420.0 nM 6.38
CHEMBL4290189 — IC50 = 470.0 nM 6.33
CHEMBL4286370 — IC50 = 480.0 nM 6.32
CHEMBL4295175 — IC50 = 930.0 nM 6.03
CHEMBL4293482 — IC50 = 1000.0 nM 6.00
CHEMBL4285014 — IC50 = 1100.0 nM 5.96
CHEMBL4282998 — IC50 = 1100.0 nM 5.96
CHEMBL4276863 — IC50 = 1200.0 nM 5.92
CHEMBL4288323 — IC50 = 1200.0 nM 5.92
CHEMBL4285042 — IC50 = 1300.0 nM 5.89
CHEMBL4277099 — IC50 = 1300.0 nM 5.89
CHEMBL4280523 — IC50 = 1300.0 nM 5.89
CHEMBL4294556 — IC50 = 1400.0 nM 5.85
CHEMBL4287238 — IC50 = 2500.0 nM 5.60
CHEMBL4280418 — IC50 = 2800.0 nM 5.55
CHEMBL4287505 — IC50 = 2800.0 nM 5.55
CHEMBL4291528 — IC50 = 2800.0 nM 5.55
CHEMBL4280297 — IC50 = 4400.0 nM 5.36
CHEMBL4292627 — IC50 = 4500.0 nM 5.35
CHEMBL4285642 — IC50 = 4700.0 nM 5.33
CHEMBL4290647 — IC50 = 6300.0 nM 5.20
CHEMBL4285366 — IC50 = 6500.0 nM 5.19
CHEMBL4293188 — IC50 = 7400.0 nM 5.13
CHEMBL4280010 — IC50 = 7800.0 nM 5.11
CHEMBL4282330 — IC50 = 9100.0 nM 5.04
CHEMBL4287328 — IC50 = 9100.0 nM 5.04
CHEMBL4292011 — IC50 = 11000.0 nM 4.96
CHEMBL4276682 — IC50 = 11000.0 nM 4.96
CHEMBL4291735 — IC50 = 13000.0 nM 4.89
CHEMBL4287529 — IC50 = 15000.0 nM 4.82
CHEMBL4283881 — IC50 = 16000.0 nM 4.80