Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4630006

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

Binding
Inhibition of human JAK3 (780 to end residues) expressed in baculovirus infected Sf9 cells using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method
ChEMBL ↗
67
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase JAK3 (CHEMBL2148) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
Noji S, Hara Y, Miura T, Yamanaka H, Maeda K, Hori A, Yamamoto H, Obika S, Inoue M, Hase Y, Orita T, Doi S, Adachi T, Tanimoto A, Oki C, Kimoto Y, Ogawa Y, Negoro T, Hashimoto H, Shiozaki M.
J Med Chem (2020) 63 : 7163 -7185
PubMed 32511913 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 67 6.96 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL221959 TOFACITINIB 4.0 1 8.96
CHEMBL3689514 — — 2 8.40
CHEMBL3689517 — — 2 8.22
CHEMBL3693599 — — 1 8.00
CHEMBL3689516 — — 2 7.96
CHEMBL3689519 — — 2 7.96
CHEMBL4297507 DELGOCITINIB 3.0 1 7.89
CHEMBL4646256 — — 1 7.75
CHEMBL3689515 — — 2 7.72
CHEMBL3689518 — — 1 7.68
CHEMBL3693624 — — 1 7.39
CHEMBL4639774 — — 1 7.36
CHEMBL3693620 — — 1 7.32
CHEMBL4635108 — — 1 7.28
CHEMBL3689522 — — 1 7.24
CHEMBL4639676 — — 1 7.21
CHEMBL3693592 — — 1 7.17
CHEMBL4644221 — — 1 7.14
CHEMBL4640920 — — 1 7.11
CHEMBL1630770 — — 1 7.10
CHEMBL4632611 — — 1 7.09
CHEMBL3693628 — — 1 7.06
CHEMBL4637879 — — 1 7.03
CHEMBL4639538 — — 1 6.96
CHEMBL4634866 — — 1 6.96
CHEMBL4637363 — — 1 6.92
CHEMBL3689526 — — 1 6.89
CHEMBL4635687 — — 1 6.89
CHEMBL4632796 — — 1 6.85
CHEMBL1630766 — — 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL221959 TOFACITINIB IC50 = 1.1 nM 8.96
CHEMBL3689514 — IC50 = 4.0 nM 8.40
CHEMBL3689517 — IC50 = 6.0 nM 8.22
CHEMBL3689517 — IC50 = 6.4 nM 8.19
CHEMBL3689514 — IC50 = 7.0 nM 8.15
CHEMBL3693599 — IC50 = 10.0 nM 8.00
CHEMBL3689516 — IC50 = 11.0 nM 7.96
CHEMBL3689519 — IC50 = 11.0 nM 7.96
CHEMBL3689516 — IC50 = 11.0 nM 7.96
CHEMBL4297507 DELGOCITINIB IC50 = 13.0 nM 7.89
CHEMBL4646256 — IC50 = 18.0 nM 7.75
CHEMBL3689515 — IC50 = 19.0 nM 7.72
CHEMBL3689518 — IC50 = 21.0 nM 7.68
CHEMBL3689519 — IC50 = 36.0 nM 7.44
CHEMBL3689515 — IC50 = 38.0 nM 7.42
CHEMBL3693624 — IC50 = 41.0 nM 7.39
CHEMBL4639774 — IC50 = 44.0 nM 7.36
CHEMBL3693620 — IC50 = 48.0 nM 7.32
CHEMBL4635108 — IC50 = 53.0 nM 7.28
CHEMBL3689522 — IC50 = 58.0 nM 7.24
CHEMBL4639676 — IC50 = 61.0 nM 7.21
CHEMBL3693592 — IC50 = 67.0 nM 7.17
CHEMBL4644221 — IC50 = 73.0 nM 7.14
CHEMBL4640920 — IC50 = 77.0 nM 7.11
CHEMBL1630770 — IC50 = 79.0 nM 7.10
CHEMBL4632611 — IC50 = 82.0 nM 7.09
CHEMBL3693628 — IC50 = 88.0 nM 7.06
CHEMBL4637879 — IC50 = 94.0 nM 7.03
CHEMBL4639538 — IC50 = 110.0 nM 6.96
CHEMBL4634866 — IC50 = 110.0 nM 6.96
CHEMBL4637363 — IC50 = 120.0 nM 6.92
CHEMBL3689526 — IC50 = 130.0 nM 6.89
CHEMBL4635687 — IC50 = 130.0 nM 6.89
CHEMBL4632796 — IC50 = 140.0 nM 6.85
CHEMBL1630766 — IC50 = 160.0 nM 6.80
CHEMBL3693596 — IC50 = 170.0 nM 6.77
CHEMBL3693618 — IC50 = 180.0 nM 6.75
CHEMBL4643358 — IC50 = 200.0 nM 6.70
CHEMBL4636510 — IC50 = 210.0 nM 6.68
CHEMBL3693625 — IC50 = 250.0 nM 6.60
CHEMBL4645765 — IC50 = 260.0 nM 6.58
CHEMBL3969009 — IC50 = 300.0 nM 6.52
CHEMBL4648694 — IC50 = 330.0 nM 6.48
CHEMBL4649779 — IC50 = 400.0 nM 6.40
CHEMBL3689524 — IC50 = 410.0 nM 6.39
CHEMBL4649366 — IC50 = 410.0 nM 6.39
CHEMBL4646093 — IC50 = 420.0 nM 6.38
CHEMBL4639731 — IC50 = 640.0 nM 6.19
CHEMBL4638316 — IC50 = 660.0 nM 6.18
CHEMBL4641927 — IC50 = 790.0 nM 6.10