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Assay Detail

CHEMBL5164796

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Functional
Antiproliferative activity against human KM12-Luc cells assessed as inhibition of cell growth incubated for 3 days by CCK8 assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KM12-Luc
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance.
Wang Z, Wang J, Wang Y, Xiang S, Song X, Tu Z, Zhou Y, Zhang ZM, Zhang Z, Ding K, Lu X.
J Med Chem (2022) 65 : 6325 -6337
PubMed 35426680 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.23 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4297627 SELITRECTINIB 2.0 1 8.64
CHEMBL5195469 1 7.81
CHEMBL3889654 LAROTRECTINIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4297627 SELITRECTINIB IC50 = 2.3 nM 8.64
CHEMBL5195469 IC50 = 15.5 nM 7.81
CHEMBL3889654 LAROTRECTINIB IC50 - -