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Assay Detail

CHEMBL5501739

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Binding
Inhibition of human TLK2 preincubated for 20 mins followed by 33P-ATP addition and measured after 120 mins by hotspot assay
ChEMBL ↗
96
Total Activities
96
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

Serine/threonine-protein kinase tousled-like 2 (CHEMBL5404) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and optimization of narrow spectrum inhibitors of Tousled like kinase 2 (TLK2) using quantitative structure activity relationships.
Asquith CRM, East MP, Laitinen T, Alamillo-Ferrer C, Hartikainen E, Wells CI, Axtman AD, Drewry DH, Tizzard GJ, Poso A, Willson TM, Johnson GL.
Eur J Med Chem (2024) 271 : 116357 -116357
PubMed 38636130 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 96 6.57 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5549938 — — 1 8.04
CHEMBL5505789 — — 1 7.92
CHEMBL5555013 — — 1 7.82
CHEMBL5505914 — — 1 7.82
CHEMBL5555697 — — 1 7.75
CHEMBL5556475 — — 1 7.64
CHEMBL5505934 — — 1 7.58
CHEMBL5556322 — — 1 7.57
CHEMBL5523411 — — 1 7.47
CHEMBL5512470 — — 1 7.44
CHEMBL5556177 — — 1 7.34
CHEMBL5559472 — — 1 7.33
CHEMBL5518017 — — 1 7.32
CHEMBL107225 — — 1 7.21
CHEMBL5542619 — — 1 7.17
CHEMBL5558307 — — 1 7.11
CHEMBL5517951 — — 1 7.06
CHEMBL5555801 — — 1 7.02
CHEMBL5555012 — — 1 7.00
CHEMBL5555855 — — 1 7.00
CHEMBL5559206 — — 1 7.00
CHEMBL5555911 — — 1 6.96
CHEMBL5556090 — — 1 6.96
CHEMBL5523653 — — 1 6.96
CHEMBL5505767 — — 1 6.92
CHEMBL5542185 — — 1 6.92
CHEMBL5558654 — — 1 6.89
CHEMBL5517792 — — 1 6.89
CHEMBL5505761 — — 1 6.85
CHEMBL5518089 — — 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5549938 — IC50 = 9.1 nM 8.04
CHEMBL5505789 — IC50 = 12.0 nM 7.92
CHEMBL5505914 — IC50 = 15.0 nM 7.82
CHEMBL5555013 — IC50 = 15.0 nM 7.82
CHEMBL5555697 — IC50 = 18.0 nM 7.75
CHEMBL5556475 — IC50 = 23.0 nM 7.64
CHEMBL5505934 — IC50 = 26.0 nM 7.58
CHEMBL5556322 — IC50 = 27.0 nM 7.57
CHEMBL5523411 — IC50 = 34.0 nM 7.47
CHEMBL5512470 — IC50 = 36.0 nM 7.44
CHEMBL5556177 — IC50 = 46.0 nM 7.34
CHEMBL5559472 — IC50 = 47.0 nM 7.33
CHEMBL5518017 — IC50 = 48.0 nM 7.32
CHEMBL107225 — IC50 = 62.0 nM 7.21
CHEMBL5542619 — IC50 = 67.0 nM 7.17
CHEMBL5558307 — IC50 = 77.0 nM 7.11
CHEMBL5517951 — IC50 = 88.0 nM 7.06
CHEMBL5555801 — IC50 = 95.0 nM 7.02
CHEMBL5555012 — IC50 = 100.0 nM 7.00
CHEMBL5555855 — IC50 = 100.0 nM 7.00
CHEMBL5559206 — IC50 = 100.0 nM 7.00
CHEMBL5555911 — IC50 = 110.0 nM 6.96
CHEMBL5556090 — IC50 = 110.0 nM 6.96
CHEMBL5523653 — IC50 = 110.0 nM 6.96
CHEMBL5542185 — IC50 = 120.0 nM 6.92
CHEMBL5505767 — IC50 = 120.0 nM 6.92
CHEMBL5558654 — IC50 = 130.0 nM 6.89
CHEMBL5517792 — IC50 = 130.0 nM 6.89
CHEMBL5505761 — IC50 = 140.0 nM 6.85
CHEMBL5518089 — IC50 = 140.0 nM 6.85
CHEMBL5559521 — IC50 = 150.0 nM 6.82
CHEMBL5523551 — IC50 = 150.0 nM 6.82
CHEMBL5523586 — IC50 = 160.0 nM 6.80
CHEMBL5542171 — IC50 = 170.0 nM 6.77
CHEMBL5556812 — IC50 = 180.0 nM 6.75
CHEMBL5505927 — IC50 = 190.0 nM 6.72
CHEMBL5542948 — IC50 = 190.0 nM 6.72
CHEMBL5556132 — IC50 = 200.0 nM 6.70
CHEMBL5556373 — IC50 = 220.0 nM 6.66
CHEMBL5555777 — IC50 = 230.0 nM 6.64
CHEMBL258805 SU-9516 IC50 = 240.0 nM 6.62
CHEMBL5555927 — IC50 = 250.0 nM 6.60
CHEMBL5556148 — IC50 = 260.0 nM 6.58
CHEMBL5505743 — IC50 = 330.0 nM 6.48
CHEMBL5558519 — IC50 = 340.0 nM 6.47
CHEMBL5517654 — IC50 = 340.0 nM 6.47
CHEMBL5555831 — IC50 = 340.0 nM 6.47
CHEMBL5505937 — IC50 = 380.0 nM 6.42
CHEMBL5558111 — IC50 = 400.0 nM 6.40
CHEMBL5558186 — IC50 = 440.0 nM 6.36