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Assay Detail

CHEMBL5327932

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

Binding
Binding affinity to human wild type TYK2 JH2 domain (G556/D888) expressed in mammalian expression system
ChEMBL ↗
41
Total Activities
41
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

Non-receptor tyrosine-protein kinase TYK2 (CHEMBL3553) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Potent and Selective Tyrosine Kinase 2 Inhibitor: TAK-279.
Leit S, Greenwood J, Carriero S, Mondal S, Abel R, Ashwell M, Blanchette H, Boyles NA, Cartwright M, Collis A, Feng S, Ghanakota P, Harriman GC, Hosagrahara V, Kaila N, Kapeller R, Rafi SB, Romero DL, Tarantino PM, Timaniya J, Toms AV, Wester RT, Westlin W, Srivastava B, Miao W, Tummino P, McElwee JJ, Edmondson SD, Masse CE.
J Med Chem (2023) 66 : 10473 -10496
PubMed 37427891 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 41 9.96 10.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5433700 — — 1 10.72
CHEMBL5398548 — — 1 10.64
CHEMBL5407138 — — 1 10.48
CHEMBL5430689 — — 1 10.47
CHEMBL5415951 — — 1 10.41
CHEMBL5404091 — — 1 10.20
CHEMBL5405569 — — 1 10.17
CHEMBL5422880 — — 1 10.14
CHEMBL5420172 — — 1 10.11
CHEMBL5396767 — — 1 10.07
CHEMBL5424640 — — 1 10.06
CHEMBL5399515 — — 1 10.00
CHEMBL5401172 — — 1 9.98
CHEMBL5423799 — — 1 9.89
CHEMBL5432382 — — 1 9.70
CHEMBL5427213 — — 1 9.51
CHEMBL5405274 — — 1 9.42
CHEMBL5419398 — — 1 9.34
CHEMBL5437915 — — 1 9.32
CHEMBL5425044 — — 1 8.57
CHEMBL5427850 — — 1 -
CHEMBL5431732 — — 1 -
CHEMBL5425400 — — 1 -
CHEMBL5436767 — — 1 -
CHEMBL5403825 — — 1 -
CHEMBL5438635 — — 1 -
CHEMBL5440491 — — 1 -
CHEMBL5411775 — — 1 -
CHEMBL5414946 — — 1 -
CHEMBL5419281 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5433700 — Kd = 0.019 nM 10.72
CHEMBL5398548 — Kd = 0.023 nM 10.64
CHEMBL5407138 — Kd = 0.033 nM 10.48
CHEMBL5430689 — Kd = 0.034 nM 10.47
CHEMBL5415951 — Kd = 0.039 nM 10.41
CHEMBL5404091 — Kd = 0.063 nM 10.20
CHEMBL5405569 — Kd = 0.068 nM 10.17
CHEMBL5422880 — Kd = 0.073 nM 10.14
CHEMBL5420172 — Kd = 0.078 nM 10.11
CHEMBL5396767 — Kd = 0.086 nM 10.07
CHEMBL5424640 — Kd = 0.088 nM 10.06
CHEMBL5399515 — Kd = 0.099 nM 10.00
CHEMBL5401172 — Kd = 0.105 nM 9.98
CHEMBL5423799 — Kd = 0.13 nM 9.89
CHEMBL5432382 — Kd = 0.2 nM 9.70
CHEMBL5427213 — Kd = 0.31 nM 9.51
CHEMBL5405274 — Kd = 0.38 nM 9.42
CHEMBL5419398 — Kd = 0.46 nM 9.34
CHEMBL5437915 — Kd = 0.48 nM 9.32
CHEMBL5425044 — Kd = 2.7 nM 8.57
CHEMBL5396334 — Kd = 0.003 nM -
CHEMBL5397381 — Kd = 0.004 nM -
CHEMBL5422616 — Kd = 0.004 nM -
CHEMBL5414602 — Kd = 0.002 nM -
CHEMBL5423859 — Kd = 0.001 nM -
CHEMBL5418744 — Kd = 0.003 nM -
CHEMBL5402351 — Kd = 0.008 nM -
CHEMBL5398529 — Kd = 0.006 nM -
CHEMBL5428288 — Kd = 0.005 nM -
CHEMBL5414851 — Kd = 0.007 nM -
CHEMBL5440397 — Kd = 0.001 nM -
CHEMBL5419281 — Kd = 0.002 nM -
CHEMBL5414946 — Kd = 0.004 nM -
CHEMBL5411775 — Kd = 0.006 nM -
CHEMBL5440491 — Kd = 0.004 nM -
CHEMBL5438635 — Kd = 0.004 nM -
CHEMBL5403825 — Kd = 0.003 nM -
CHEMBL5436767 — Kd = 0.002 nM -
CHEMBL5425400 — Kd = 0.002 nM -
CHEMBL5431732 — Kd = 0.006 nM -
CHEMBL5427850 — Kd = 0.002 nM -