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Assay Detail

CHEMBL5235544

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

Binding
Inhibition of DYRK1A (unknown origin)
18
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

β-Carboline as a Privileged Scaffold for Multitarget Strategies in Alzheimer's Disease Therapy.
Beato A, Gori A, Boucherle B, Peuchmaur M, Haudecoeur R.
J Med Chem (2021) 64 : 1392 -1422
PubMed 33528252 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.75 7.66
IC5 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269538 HARMINE 1.0 1 7.66
CHEMBL4474836 1 7.60
CHEMBL44889 2 7.46
CHEMBL4460242 1 7.46
CHEMBL325351 1 7.46
CHEMBL4514653 1 7.46
CHEMBL4159941 1 7.25
CHEMBL5289480 1 7.25
CHEMBL4066450 1 7.25
CHEMBL5267999 1 5.70
CHEMBL5286216 1 5.70
CHEMBL5279996 1 5.70
CHEMBL340807 HARMALINE 1 5.34
CHEMBL5276049 1 4.57
CHEMBL5280284 1 -
CHEMBL12014 HARMAN 1 -
CHEMBL275224 NORHARMANE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269538 HARMINE IC50 = 22.0 nM 7.66
CHEMBL4474836 IC50 = 25.0 nM 7.60
CHEMBL44889 IC50 = 35.0 nM 7.46
CHEMBL4460242 IC50 = 35.0 nM 7.46
CHEMBL325351 IC50 = 35.0 nM 7.46
CHEMBL4514653 IC50 = 35.0 nM 7.46
CHEMBL44889 IC50 = 48.0 nM 7.32
CHEMBL4159941 IC50 = 56.0 nM 7.25
CHEMBL5289480 IC50 = 56.0 nM 7.25
CHEMBL4066450 IC50 = 56.0 nM 7.25
CHEMBL5286216 IC50 = 2000.0 nM 5.70
CHEMBL5279996 IC50 = 2000.0 nM 5.70
CHEMBL5267999 IC50 = 2000.0 nM 5.70
CHEMBL340807 HARMALINE IC50 = 4600.0 nM 5.34
CHEMBL5276049 IC50 = 27000.0 nM 4.57
CHEMBL5280284 IC5 = 0.2 uM -
CHEMBL12014 HARMAN IC50 > 1800.0 nM -
CHEMBL275224 NORHARMANE IC50 > 1800.0 nM -