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Assay Detail

CHEMBL4666929

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

Binding
Inhibition of recombinant human JAK1 (854 to 1154 residues) expressed in insect cells using Y1-B as substrate incubated for 30 mins by microfluidic mobility shift assay
ChEMBL ↗
57
Total Activities
57
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

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
Ki 57 8.77 10.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4746726 — — 1 10.12
CHEMBL4789075 — — 1 9.96
CHEMBL4742159 — — 1 9.92
CHEMBL4764019 — — 1 9.82
CHEMBL4740778 — — 1 9.72
CHEMBL4793262 — — 1 9.68
CHEMBL4777342 — — 1 9.68
CHEMBL4744172 — — 1 9.68
CHEMBL4746416 — — 1 9.54
CHEMBL4755725 — — 1 9.52
CHEMBL4740223 — — 1 9.51
CHEMBL4745474 — — 1 9.51
CHEMBL4750979 — — 1 9.34
CHEMBL4788860 — — 1 9.33
CHEMBL4780070 — — 1 9.29
CHEMBL4757833 — — 1 9.28
CHEMBL4756876 — — 1 9.25
CHEMBL4760562 — — 1 9.25
CHEMBL2178801 — — 1 9.24
CHEMBL4788474 — — 1 9.22
CHEMBL221959 TOFACITINIB 4.0 1 9.19
CHEMBL4742382 — — 1 9.17
CHEMBL4798728 — — 1 9.15
CHEMBL4778284 — — 1 9.07
CHEMBL4784721 — — 1 9.05
CHEMBL3622821 UPADACITINIB 4.0 1 9.05
CHEMBL4800012 — — 1 9.05
CHEMBL4756764 — — 1 9.04
CHEMBL4794915 — — 1 9.02
CHEMBL4760406 — — 1 9.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4746726 — Ki = 0.075 nM 10.12
CHEMBL4789075 — Ki = 0.11 nM 9.96
CHEMBL4742159 — Ki = 0.12 nM 9.92
CHEMBL4764019 — Ki = 0.15 nM 9.82
CHEMBL4740778 — Ki = 0.19 nM 9.72
CHEMBL4793262 — Ki = 0.21 nM 9.68
CHEMBL4777342 — Ki = 0.21 nM 9.68
CHEMBL4744172 — Ki = 0.21 nM 9.68
CHEMBL4746416 — Ki = 0.29 nM 9.54
CHEMBL4755725 — Ki = 0.3 nM 9.52
CHEMBL4740223 — Ki = 0.31 nM 9.51
CHEMBL4745474 — Ki = 0.31 nM 9.51
CHEMBL4750979 — Ki = 0.46 nM 9.34
CHEMBL4788860 — Ki = 0.47 nM 9.33
CHEMBL4780070 — Ki = 0.51 nM 9.29
CHEMBL4757833 — Ki = 0.53 nM 9.28
CHEMBL4756876 — Ki = 0.56 nM 9.25
CHEMBL4760562 — Ki = 0.56 nM 9.25
CHEMBL2178801 — Ki = 0.57 nM 9.24
CHEMBL4788474 — Ki = 0.6 nM 9.22
CHEMBL221959 TOFACITINIB Ki = 0.64 nM 9.19
CHEMBL4742382 — Ki = 0.67 nM 9.17
CHEMBL4798728 — Ki = 0.71 nM 9.15
CHEMBL4778284 — Ki = 0.85 nM 9.07
CHEMBL4800012 — Ki = 0.89 nM 9.05
CHEMBL3622821 UPADACITINIB Ki = 0.89 nM 9.05
CHEMBL4784721 — Ki = 0.9 nM 9.05
CHEMBL4756764 — Ki = 0.91 nM 9.04
CHEMBL4794915 — Ki = 0.95 nM 9.02
CHEMBL4760406 — Ki = 0.99 nM 9.00
CHEMBL3667519 — Ki = 0.99 nM 9.00
CHEMBL4762168 — Ki = 1.3 nM 8.89
CHEMBL4781087 — Ki = 1.4 nM 8.85
CHEMBL4760135 — Ki = 1.4 nM 8.85
CHEMBL4778449 — Ki = 1.8 nM 8.74
CHEMBL4795297 — Ki = 1.9 nM 8.72
CHEMBL4790609 — Ki = 2.1 nM 8.68
CHEMBL4755407 — Ki = 2.2 nM 8.66
CHEMBL2178799 — Ki = 2.8 nM 8.55
CHEMBL2386653 — Ki = 2.9 nM 8.54
CHEMBL4757212 — Ki = 3.3 nM 8.48
CHEMBL4764700 — Ki = 3.9 nM 8.41
CHEMBL4781423 — Ki = 4.3 nM 8.37
CHEMBL4791878 — Ki = 5.6 nM 8.25
CHEMBL4745011 — Ki = 5.7 nM 8.24
CHEMBL4755436 — Ki = 7.8 nM 8.11
CHEMBL4794314 — Ki = 7.9 nM 8.10
CHEMBL4796325 — Ki = 9.2 nM 8.04
CHEMBL4742670 — Ki = 12.0 nM 7.92
CHEMBL4076947 — Ki = 23.0 nM 7.64