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Assay Detail

CHEMBL4666933

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Binding
Inhibition of JAK in human BEAS-2B cells assessed as reduction in IL13-induced STAT6 phosphorylation incubated for 1 hr followed by IL13 addition and measured after 15 mins by immunofluorescence assay
ChEMBL ↗
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BEAS-2B
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Janus Kinase (JAK) (CHEMBL2363062) ↗
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.
Zak M,Hanan EJ,Lupardus P,Brown DG,Robinson C,Siu M,Lyssikatos JP,Romero FA,Zhao G,Kellar T,Mendonca R,Ray NC,Goodacre SC,Crackett PH,McLean N,Hurley CA,Yuen PW,Cheng YX,Liu X,Liimatta M,Kohli PB,Nonomiya J,Salmon G,Buckley G,Lloyd J,Gibbons P,Ghilardi N,Kenny JR,Johnson A
Bioorg Med Chem Lett (2019) 29 : 1522 -1531
PubMed 30981576 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 57 7.57 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4764019 — — 1 8.55
CHEMBL4742159 — — 1 8.48
CHEMBL4740778 — — 1 8.40
CHEMBL4777342 — — 1 8.33
CHEMBL4793262 — — 1 8.30
CHEMBL4744172 — — 1 8.28
CHEMBL4745474 — — 1 8.19
CHEMBL4780070 — — 1 8.04
CHEMBL4750979 — — 1 7.96
CHEMBL4757833 — — 1 7.89
CHEMBL4746416 — — 1 7.89
CHEMBL4742382 — — 1 7.85
CHEMBL4756876 — — 1 7.85
CHEMBL4794915 — — 1 7.82
CHEMBL4760562 — — 1 7.75
CHEMBL4788474 — — 1 7.70
CHEMBL4788860 — — 1 7.70
CHEMBL4762168 — — 1 7.68
CHEMBL4784721 — — 1 7.66
CHEMBL4800012 — — 1 7.64
CHEMBL2178801 — — 1 7.60
CHEMBL4778284 — — 1 7.58
CHEMBL4760135 — — 1 7.57
CHEMBL4798728 — — 1 7.47
CHEMBL4760406 — — 1 7.47
CHEMBL4789075 — — 1 7.44
CHEMBL4778449 — — 1 7.44
CHEMBL4795297 — — 1 7.42
CHEMBL221959 TOFACITINIB 4.0 1 7.41
CHEMBL4746726 — — 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4764019 — IC50 = 2.8 nM 8.55
CHEMBL4742159 — IC50 = 3.3 nM 8.48
CHEMBL4740778 — IC50 = 4.0 nM 8.40
CHEMBL4777342 — IC50 = 4.7 nM 8.33
CHEMBL4793262 — IC50 = 5.0 nM 8.30
CHEMBL4744172 — IC50 = 5.2 nM 8.28
CHEMBL4745474 — IC50 = 6.4 nM 8.19
CHEMBL4780070 — IC50 = 9.2 nM 8.04
CHEMBL4750979 — IC50 = 11.0 nM 7.96
CHEMBL4757833 — IC50 = 13.0 nM 7.89
CHEMBL4746416 — IC50 = 13.0 nM 7.89
CHEMBL4742382 — IC50 = 14.0 nM 7.85
CHEMBL4756876 — IC50 = 14.0 nM 7.85
CHEMBL4794915 — IC50 = 15.0 nM 7.82
CHEMBL4760562 — IC50 = 18.0 nM 7.75
CHEMBL4788474 — IC50 = 20.0 nM 7.70
CHEMBL4788860 — IC50 = 20.0 nM 7.70
CHEMBL4762168 — IC50 = 21.0 nM 7.68
CHEMBL4784721 — IC50 = 22.0 nM 7.66
CHEMBL4800012 — IC50 = 23.0 nM 7.64
CHEMBL2178801 — IC50 = 25.0 nM 7.60
CHEMBL4778284 — IC50 = 26.0 nM 7.58
CHEMBL4760135 — IC50 = 27.0 nM 7.57
CHEMBL4798728 — IC50 = 34.0 nM 7.47
CHEMBL4760406 — IC50 = 34.0 nM 7.47
CHEMBL4789075 — IC50 = 36.0 nM 7.44
CHEMBL4778449 — IC50 = 36.0 nM 7.44
CHEMBL4795297 — IC50 = 38.0 nM 7.42
CHEMBL221959 TOFACITINIB IC50 = 39.0 nM 7.41
CHEMBL4746726 — IC50 = 40.0 nM 7.40
CHEMBL4791878 — IC50 = 42.0 nM 7.38
CHEMBL4755407 — IC50 = 42.0 nM 7.38
CHEMBL3622821 UPADACITINIB IC50 = 45.0 nM 7.35
CHEMBL4781087 — IC50 = 54.0 nM 7.27
CHEMBL3667519 — IC50 = 58.0 nM 7.24
CHEMBL4790609 — IC50 = 64.0 nM 7.19
CHEMBL4781423 — IC50 = 93.0 nM 7.03
CHEMBL4740223 — IC50 = 140.0 nM 6.85
CHEMBL2386653 — IC50 = 210.0 nM 6.68
CHEMBL2178799 — IC50 = 230.0 nM 6.64
CHEMBL4755725 — IC50 = 370.0 nM 6.43
CHEMBL4076947 — IC50 = 1300.0 nM 5.89
CHEMBL4796325 — IC50 - — -
CHEMBL2178806 — IC50 - — -
CHEMBL4748712 — IC50 - — -
CHEMBL2178252 — IC50 > 1000.0 nM -
CHEMBL4786888 — IC50 > 1000.0 nM -
CHEMBL4780485 — IC50 - — -
CHEMBL4757212 — IC50 - — -
CHEMBL4742670 — IC50 - — -