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Assay Detail

CHEMBL5156818

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

Binding
Inhibition of recombinant human TTBK1 using RICDLHDDEEDEAMSITA as substrate incubated for 30 mins in presence of 33P-gamma-ATP
ChEMBL ↗
50
Total Activities
50
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

Tau-tubulin kinase 1 (CHEMBL1926492) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

TDP-43 Modulation by Tau-Tubulin Kinase 1 Inhibitors: A New Avenue for Future Amyotrophic Lateral Sclerosis Therapy.
Nozal V, Martínez-González L, Gomez-Almeria M, Gonzalo-Consuegra C, Santana P, Chaikuad A, Pérez-Cuevas E, Knapp S, Lietha D, Ramírez D, Petralla S, Monti B, Gil C, Martín-Requero A, Palomo V, de Lago E, Martinez A, Martinez A.
J Med Chem (2022) 65 : 1585 -1607
PubMed 34978799 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 5.84 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5204869 — — 1 6.62
CHEMBL5200069 — — 1 6.48
CHEMBL5193488 — — 1 6.47
CHEMBL5181249 — — 1 6.44
CHEMBL5184336 — — 1 6.43
CHEMBL5180098 — — 1 6.42
CHEMBL5178965 — — 1 6.41
CHEMBL5198544 — — 1 6.41
CHEMBL5209196 — — 1 6.38
CHEMBL5187459 — — 1 6.36
CHEMBL5187125 — — 1 6.35
CHEMBL5197012 — — 1 6.32
CHEMBL5171328 — — 1 6.28
CHEMBL5185704 — — 1 6.28
CHEMBL5193034 — — 1 6.21
CHEMBL5188513 — — 1 6.19
CHEMBL5200160 — — 1 6.12
CHEMBL5197789 — — 1 6.12
CHEMBL5206548 — — 1 6.12
CHEMBL5208565 — — 1 6.11
CHEMBL5207783 — — 1 6.10
CHEMBL5196033 — — 1 6.08
CHEMBL1257781 — — 1 6.00
CHEMBL5178462 — — 1 6.00
CHEMBL5179559 — — 1 5.99
CHEMBL5178871 — — 1 5.88
CHEMBL5202436 — — 1 5.82
CHEMBL5209161 — — 1 5.82
CHEMBL5192144 — — 1 5.81
CHEMBL5182006 — — 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5204869 — IC50 = 240.0 nM 6.62
CHEMBL5200069 — IC50 = 330.0 nM 6.48
CHEMBL5193488 — IC50 = 340.0 nM 6.47
CHEMBL5181249 — IC50 = 360.0 nM 6.44
CHEMBL5184336 — IC50 = 370.0 nM 6.43
CHEMBL5180098 — IC50 = 380.0 nM 6.42
CHEMBL5178965 — IC50 = 390.0 nM 6.41
CHEMBL5198544 — IC50 = 390.0 nM 6.41
CHEMBL5209196 — IC50 = 420.0 nM 6.38
CHEMBL5187459 — IC50 = 440.0 nM 6.36
CHEMBL5187125 — IC50 = 450.0 nM 6.35
CHEMBL5197012 — IC50 = 480.0 nM 6.32
CHEMBL5171328 — IC50 = 520.0 nM 6.28
CHEMBL5185704 — IC50 = 520.0 nM 6.28
CHEMBL5193034 — IC50 = 610.0 nM 6.21
CHEMBL5188513 — IC50 = 650.0 nM 6.19
CHEMBL5200160 — IC50 = 750.0 nM 6.12
CHEMBL5197789 — IC50 = 750.0 nM 6.12
CHEMBL5206548 — IC50 = 750.0 nM 6.12
CHEMBL5208565 — IC50 = 770.0 nM 6.11
CHEMBL5207783 — IC50 = 790.0 nM 6.10
CHEMBL5196033 — IC50 = 840.0 nM 6.08
CHEMBL1257781 — IC50 = 1000.0 nM 6.00
CHEMBL5178462 — IC50 = 990.0 nM 6.00
CHEMBL5179559 — IC50 = 1020.0 nM 5.99
CHEMBL5178871 — IC50 = 1320.0 nM 5.88
CHEMBL5209161 — IC50 = 1500.0 nM 5.82
CHEMBL5202436 — IC50 = 1500.0 nM 5.82
CHEMBL5192144 — IC50 = 1550.0 nM 5.81
CHEMBL5182006 — IC50 = 1580.0 nM 5.80
CHEMBL5193908 — IC50 = 1710.0 nM 5.77
CHEMBL4517951 — IC50 = 2200.0 nM 5.66
CHEMBL5207918 — IC50 = 2200.0 nM 5.66
CHEMBL5208571 — IC50 = 2300.0 nM 5.64
CHEMBL5169390 — IC50 = 2300.0 nM 5.64
CHEMBL5203204 — IC50 = 2720.0 nM 5.57
CHEMBL5186693 — IC50 = 3000.0 nM 5.52
CHEMBL5186860 — IC50 = 3200.0 nM 5.50
CHEMBL5193008 — IC50 = 3560.0 nM 5.45
CHEMBL5209114 — IC50 = 4300.0 nM 5.37
CHEMBL5171736 — IC50 = 4700.0 nM 5.33
CHEMBL5198629 — IC50 = 4900.0 nM 5.31
CHEMBL5177584 — IC50 = 5030.0 nM 5.30
CHEMBL5182026 — IC50 = 5610.0 nM 5.25
CHEMBL5204443 — IC50 = 6100.0 nM 5.21
CHEMBL5183323 — IC50 = 9150.0 nM 5.04
CHEMBL5177393 — IC50 = 12800.0 nM 4.89
CHEMBL5186604 — IC50 = 15200.0 nM 4.82
CHEMBL5201662 — IC50 = 18200.0 nM 4.74
CHEMBL5209148 — IC50 = 21800.0 nM 4.66