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Assay Detail

CHEMBL4689210

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

ADMET
Cytotoxicity against human Fibroblast cells assessed as reduction in cell viability incubated for 48 hrs by Hoechst-33342 staining based cell counting method (Rvb > 25 microM)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type Fibroblast
Confidence 1 — Organism
Curated By Autocuration

Target

Fibroblast (CHEMBL5314315)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of DB18, a potent inhibitor of CLK kinases with a high selectivity against DYRK1A kinase.
Brahmaiah D,Kanaka Durga Bhavani A,Aparna P,Sampath Kumar N,Solhi H,Le Guevel R,Baratte B,Ruchaud S,Bach S,Singh Jadav S,Raji Reddy C,Roisnel T,Mosset P,Levoin N,Grée R
Bioorg Med Chem (2021) 31 : 115962 -115962
PubMed 33422908 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.63 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53463 DOXORUBICIN 4.0 1 7.82
CHEMBL428647 PACLITAXEL 4.0 1 7.00
CHEMBL14762 SELICICLIB 2.0 1 5.22
CHEMBL4761834 1 5.10
CHEMBL4795706 1 4.85
CHEMBL4754002 1 4.75
CHEMBL4783398 1 4.68
CHEMBL4751143 1 -
CHEMBL4793064 1 -
CHEMBL4760556 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53463 DOXORUBICIN IC50 = 15.0 nM 7.82
CHEMBL428647 PACLITAXEL IC50 = 100.0 nM 7.00
CHEMBL14762 SELICICLIB IC50 = 6000.0 nM 5.22
CHEMBL4761834 IC50 = 8000.0 nM 5.10
CHEMBL4795706 IC50 = 14000.0 nM 4.85
CHEMBL4754002 IC50 = 18000.0 nM 4.75
CHEMBL4783398 IC50 = 21000.0 nM 4.68
CHEMBL4751143 IC50 > 25000.0 nM -
CHEMBL4793064 IC50 > 25000.0 nM -
CHEMBL4760556 IC50 > 25000.0 nM -