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Assay Detail

CHEMBL5098263

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Functional
Antiproliferative activity against ALK-positive human KARPAS-299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KARPAS-299
Confidence 1 — Organism
Curated By Autocuration

Target

KARPAS-299 (CHEMBL2366156)
Type CELL-LINE
Organism Homo sapiens

Publication

Development of Alectinib-Based PROTACs as Novel Potent Degraders of Anaplastic Lymphoma Kinase (ALK).
Xie S, Sun Y, Liu Y, Li X, Li X, Zhong W, Zhan F, Zhu J, Yao H, Yang DH, Chen ZS, Xu J, Xu S.
J Med Chem (2021) 64 : 9120 -9140
PubMed 34176264 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.97 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4875115 1 7.38
CHEMBL3747525 1 7.34
CHEMBL1738797 ALECTINIB 4.0 1 7.33
CHEMBL4859551 1 7.30
CHEMBL4875202 1 7.18
CHEMBL5207601 1 7.01
CHEMBL5174385 1 7.00
CHEMBL5176906 1 6.97
CHEMBL4865374 1 6.97
CHEMBL5189754 1 6.96
CHEMBL5173908 1 6.94
CHEMBL5171663 1 6.92
CHEMBL5179368 1 6.92
CHEMBL4854383 1 6.61
CHEMBL5188519 1 6.56
CHEMBL5193329 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4875115 IC50 = 42.0 nM 7.38
CHEMBL3747525 IC50 = 46.0 nM 7.34
CHEMBL1738797 ALECTINIB IC50 = 47.0 nM 7.33
CHEMBL4859551 IC50 = 50.0 nM 7.30
CHEMBL4875202 IC50 = 66.0 nM 7.18
CHEMBL5207601 IC50 = 97.0 nM 7.01
CHEMBL5174385 IC50 = 101.0 nM 7.00
CHEMBL5176906 IC50 = 106.0 nM 6.97
CHEMBL4865374 IC50 = 107.0 nM 6.97
CHEMBL5189754 IC50 = 111.0 nM 6.96
CHEMBL5173908 IC50 = 114.0 nM 6.94
CHEMBL5171663 IC50 = 119.0 nM 6.92
CHEMBL5179368 IC50 = 119.0 nM 6.92
CHEMBL4854383 IC50 = 245.0 nM 6.61
CHEMBL5188519 IC50 = 275.0 nM 6.56
CHEMBL5193329 IC50 = 640.0 nM 6.19