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

CHEMBL4630008

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

Functional
Inhibition of IL2-induced human T cell proliferation preincubated for 30 mins followed by IL2 stimulation and measured after 3 days by [3H]thymidine incorporation based scintillation counting method
ChEMBL ↗
49
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type T-cell
Confidence 1 — Organism
Curated By Autocuration

Target

T-cell (CHEMBL614309) ↗
Type CELL-LINE

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 49 6.60 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4297507 DELGOCITINIB 3.0 1 8.05
CHEMBL3689514 — — 2 7.96
CHEMBL221959 TOFACITINIB 4.0 1 7.80
CHEMBL3689515 — — 2 7.77
CHEMBL3689517 — — 2 7.72
CHEMBL3689516 — — 2 7.48
CHEMBL3689518 — — 1 7.41
CHEMBL3689519 — — 2 7.39
CHEMBL3693624 — — 1 7.07
CHEMBL3689522 — — 1 7.00
CHEMBL3693628 — — 1 6.82
CHEMBL4649779 — — 1 6.82
CHEMBL3693592 — — 1 6.72
CHEMBL4639774 — — 1 6.66
CHEMBL4643358 — — 1 6.66
CHEMBL3693599 — — 1 6.66
CHEMBL3693620 — — 1 6.60
CHEMBL4646256 — — 1 6.57
CHEMBL4636510 — — 1 6.43
CHEMBL4639676 — — 1 6.35
CHEMBL4639538 — — 1 6.32
CHEMBL4649366 — — 1 6.11
CHEMBL4641927 — — 1 6.04
CHEMBL4635108 — — 1 5.89
CHEMBL4640920 — — 1 5.85
CHEMBL3969009 — — 1 5.77
CHEMBL4639731 — — 1 5.75
CHEMBL3689526 — — 1 5.70
CHEMBL4637363 — — 1 5.68
CHEMBL3693618 — — 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4297507 DELGOCITINIB IC50 = 8.9 nM 8.05
CHEMBL3689514 — IC50 = 11.0 nM 7.96
CHEMBL221959 TOFACITINIB IC50 = 16.0 nM 7.80
CHEMBL3689515 — IC50 = 17.0 nM 7.77
CHEMBL3689517 — IC50 = 19.0 nM 7.72
CHEMBL3689514 — IC50 = 32.0 nM 7.50
CHEMBL3689516 — IC50 = 33.0 nM 7.48
CHEMBL3689518 — IC50 = 39.0 nM 7.41
CHEMBL3689519 — IC50 = 41.0 nM 7.39
CHEMBL3689519 — IC50 = 48.0 nM 7.32
CHEMBL3689517 — IC50 = 48.0 nM 7.32
CHEMBL3689515 — IC50 = 51.0 nM 7.29
CHEMBL3689516 — IC50 = 55.0 nM 7.26
CHEMBL3693624 — IC50 = 86.0 nM 7.07
CHEMBL3689522 — IC50 = 100.0 nM 7.00
CHEMBL4649779 — IC50 = 150.0 nM 6.82
CHEMBL3693628 — IC50 = 150.0 nM 6.82
CHEMBL3693592 — IC50 = 190.0 nM 6.72
CHEMBL3693599 — IC50 = 220.0 nM 6.66
CHEMBL4643358 — IC50 = 220.0 nM 6.66
CHEMBL4639774 — IC50 = 220.0 nM 6.66
CHEMBL3693620 — IC50 = 250.0 nM 6.60
CHEMBL4646256 — IC50 = 270.0 nM 6.57
CHEMBL4636510 — IC50 = 370.0 nM 6.43
CHEMBL4639676 — IC50 = 450.0 nM 6.35
CHEMBL4639538 — IC50 = 480.0 nM 6.32
CHEMBL4649366 — IC50 = 780.0 nM 6.11
CHEMBL4641927 — IC50 = 920.0 nM 6.04
CHEMBL4635108 — IC50 = 1300.0 nM 5.89
CHEMBL4640920 — IC50 = 1400.0 nM 5.85
CHEMBL3969009 — IC50 = 1700.0 nM 5.77
CHEMBL4639731 — IC50 = 1800.0 nM 5.75
CHEMBL3689526 — IC50 = 2000.0 nM 5.70
CHEMBL4637363 — IC50 = 2100.0 nM 5.68
CHEMBL3693618 — IC50 = 2200.0 nM 5.66
CHEMBL4632796 — IC50 = 2400.0 nM 5.62
CHEMBL4635687 — IC50 = 2400.0 nM 5.62
CHEMBL4634866 — IC50 = 2900.0 nM 5.54
CHEMBL4637879 — IC50 = 3000.0 nM 5.52
CHEMBL4639875 — IC50 = 3200.0 nM 5.50
CHEMBL4632611 — IC50 = 3500.0 nM 5.46
CHEMBL3689524 — IC50 - — -
CHEMBL3693596 — IC50 - — -
CHEMBL3693625 — IC50 - — -
CHEMBL4645444 — IC50 > 10000.0 nM -
CHEMBL4642854 — IC50 > 10000.0 nM -
CHEMBL4638316 — IC50 > 10000.0 nM -
CHEMBL4638326 — IC50 > 10000.0 nM -
CHEMBL4644221 — IC50 > 10000.0 nM -