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Assay Detail

CHEMBL5635459

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

Binding
Inhibition of CDK5/p25 (unknown origin)
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 5/CDK5 activator 1 (CHEMBL1907600)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Hydrophobicity modulation via the substituents at positions 2 and 4 of 1,3,5-triazine to enhance therapeutic ability against Alzheimer's disease for potent serotonin 5-HT<sub>6</sub>R agents.
Sudoł-Tałaj S, Kucwaj-Brysz K, Podlewska S, Kurczab R, Satała G, Mordyl B, Głuch-Lutwin M, Wilczyńska-Zawal N, Jastrzębska-Więsek M, Czarnota-Łydka K, Kurowska K, Kubacka M, Żesławska E, Nitek W, Olejarz-Maciej A, Doroz-Płonka A, Partyka A, Latacz G, Wesołowska A, Handzlik J.
Eur J Med Chem (2023) 260 : 115756 -115756
PubMed 37657272 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.53 8.52
Ki 1 6.22 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL191336 1 8.52
CHEMBL2103840 DINACICLIB 3.0 1 7.26
CHEMBL14762 SELICICLIB 2.0 1 6.80
CHEMBL1614763 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL191336 IC50 = 3.0 nM 8.52
CHEMBL2103840 DINACICLIB IC50 = 55.0 nM 7.26
CHEMBL14762 SELICICLIB IC50 = 160.0 nM 6.80
CHEMBL1614763 Ki = 600.0 nM 6.22