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Assay Detail

CHEMBL4612619

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Binding
Inhibition of N-terminal GST-tagged human JAK1 catalytic domain (850 to 1154 residues) incubated for 40 mins in presence of TK substrate-biotin by TR-FRET assay
ChEMBL ↗
43
Total Activities
43
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

Fragment-Based Discovery of Pyrazolopyridones as JAK1 Inhibitors with Excellent Subtype Selectivity.
Hansen BB, Jepsen TH, Larsen M, Sindet R, Vifian T, Burhardt MN, Larsen J, Seitzberg JG, Carnerup MA, Jerre A, Mølck C, Lovato P, Rai S, Nasipireddy VR, Ritzén A.
J Med Chem (2020) 63 : 7008 -7032
PubMed 32462873 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 7.04 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4643061 — — 1 9.00
CHEMBL4639606 — — 1 8.68
CHEMBL4649484 — — 1 8.52
CHEMBL221959 TOFACITINIB 4.0 1 8.51
CHEMBL4636507 — — 1 8.47
CHEMBL3655081 ABROCITINIB 4.0 1 8.29
CHEMBL4639973 — — 1 8.19
CHEMBL4647115 — — 1 7.96
CHEMBL4638030 — — 1 7.96
CHEMBL4647276 — — 1 7.89
CHEMBL4632766 — — 1 7.85
CHEMBL4634289 — — 1 7.52
CHEMBL4640029 — — 1 7.50
CHEMBL4639048 — — 1 7.40
CHEMBL4640521 — — 1 7.40
CHEMBL4645814 — — 1 7.40
CHEMBL4645613 — — 1 7.36
CHEMBL4636220 — — 1 7.34
CHEMBL4648820 — — 1 7.33
CHEMBL4648612 — — 1 7.27
CHEMBL4640335 — — 1 7.14
CHEMBL4638953 — — 1 7.11
CHEMBL4632897 — — 1 6.96
CHEMBL4641076 — — 1 6.92
CHEMBL4636371 — — 1 6.89
CHEMBL4638696 — — 1 6.85
CHEMBL4633028 — — 1 6.66
CHEMBL4638808 — — 1 6.40
CHEMBL4647966 — — 1 6.34
CHEMBL4647506 — — 1 6.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4643061 — IC50 = 1.0 nM 9.00
CHEMBL4639606 — IC50 = 2.1 nM 8.68
CHEMBL4649484 — IC50 = 3.0 nM 8.52
CHEMBL221959 TOFACITINIB IC50 = 3.1 nM 8.51
CHEMBL4636507 — IC50 = 3.4 nM 8.47
CHEMBL3655081 ABROCITINIB IC50 = 5.1 nM 8.29
CHEMBL4639973 — IC50 = 6.4 nM 8.19
CHEMBL4647115 — IC50 = 11.0 nM 7.96
CHEMBL4638030 — IC50 = 11.0 nM 7.96
CHEMBL4647276 — IC50 = 13.0 nM 7.89
CHEMBL4632766 — IC50 = 14.0 nM 7.85
CHEMBL4634289 — IC50 = 30.0 nM 7.52
CHEMBL4640029 — IC50 = 32.0 nM 7.50
CHEMBL4645814 — IC50 = 40.0 nM 7.40
CHEMBL4640521 — IC50 = 40.0 nM 7.40
CHEMBL4639048 — IC50 = 40.0 nM 7.40
CHEMBL4645613 — IC50 = 44.0 nM 7.36
CHEMBL4636220 — IC50 = 46.0 nM 7.34
CHEMBL4648820 — IC50 = 47.0 nM 7.33
CHEMBL4648612 — IC50 = 54.0 nM 7.27
CHEMBL4640335 — IC50 = 72.0 nM 7.14
CHEMBL4638953 — IC50 = 78.0 nM 7.11
CHEMBL4632897 — IC50 = 110.0 nM 6.96
CHEMBL4641076 — IC50 = 120.0 nM 6.92
CHEMBL4636371 — IC50 = 130.0 nM 6.89
CHEMBL4638696 — IC50 = 140.0 nM 6.85
CHEMBL4633028 — IC50 = 220.0 nM 6.66
CHEMBL4638808 — IC50 = 400.0 nM 6.40
CHEMBL4647966 — IC50 = 460.0 nM 6.34
CHEMBL4647506 — IC50 = 490.0 nM 6.31
CHEMBL4642546 — IC50 = 490.0 nM 6.31
CHEMBL4648246 — IC50 = 500.0 nM 6.30
CHEMBL4637596 — IC50 = 730.0 nM 6.14
CHEMBL4636368 — IC50 = 820.0 nM 6.09
CHEMBL4649054 — IC50 = 2000.0 nM 5.70
CHEMBL4632980 — IC50 = 2100.0 nM 5.68
CHEMBL4635464 — IC50 = 2200.0 nM 5.66
CHEMBL4645113 — IC50 = 15000.0 nM 4.82
CHEMBL4633481 — IC50 = 16000.0 nM 4.80
CHEMBL4639898 — IC50 = 30000.0 nM 4.52
CHEMBL3731087 — IC50 > 900000.0 nM -
CHEMBL4647133 — IC50 > 500000.0 nM -
CHEMBL4638380 — IC50 > 100000.0 nM -