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Assay Detail

CHEMBL5106227

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

Functional
Antiproliferative activity against human TMD8 cells incubated for 72 hrs by CellTiter-Glo assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type TMD8
Confidence 1 — Organism
Curated By Autocuration

Target

TMD8 (CHEMBL4296503)
Type CELL-LINE
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors.
Yang M, Jiang H, Yang Z, Liu X, Sun H, Hao M, Hu J, Chen X, Jin J, Wang X.
Eur J Med Chem (2022) 241 : 114611 -114611
PubMed 35939993 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.88 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5189426 1 9.10
CHEMBL5179080 1 8.92
CHEMBL5176551 1 8.82
CHEMBL5196932 1 8.77
CHEMBL5170833 1 8.77
CHEMBL5189231 1 8.74
CHEMBL5193942 1 8.59
CHEMBL1873475 IBRUTINIB 4.0 1 8.57
CHEMBL5178389 1 8.47
CHEMBL5198455 1 8.27
CHEMBL5202754 1 8.14
CHEMBL5180302 1 8.04
CHEMBL5177044 1 7.92
CHEMBL5195504 1 7.89
CHEMBL5192748 1 7.81
CHEMBL5204458 1 7.65
CHEMBL5205889 1 7.65
CHEMBL5208265 1 7.61
CHEMBL5193597 1 7.55
CHEMBL5175574 1 7.51
CHEMBL5170025 1 7.42
CHEMBL4072833 EVOBRUTINIB 3.0 1 7.25
CHEMBL5206496 1 7.08
CHEMBL5206093 1 6.50
CHEMBL5206716 1 6.34
CHEMBL5171858 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5189426 IC50 = 0.8 nM 9.10
CHEMBL5179080 IC50 = 1.2 nM 8.92
CHEMBL5176551 IC50 = 1.5 nM 8.82
CHEMBL5196932 IC50 = 1.7 nM 8.77
CHEMBL5170833 IC50 = 1.7 nM 8.77
CHEMBL5189231 IC50 = 1.8 nM 8.74
CHEMBL5193942 IC50 = 2.6 nM 8.59
CHEMBL1873475 IBRUTINIB IC50 = 2.7 nM 8.57
CHEMBL5178389 IC50 = 3.4 nM 8.47
CHEMBL5198455 IC50 = 5.4 nM 8.27
CHEMBL5202754 IC50 = 7.2 nM 8.14
CHEMBL5180302 IC50 = 9.2 nM 8.04
CHEMBL5177044 IC50 = 12.1 nM 7.92
CHEMBL5195504 IC50 = 12.9 nM 7.89
CHEMBL5192748 IC50 = 15.6 nM 7.81
CHEMBL5204458 IC50 = 22.6 nM 7.65
CHEMBL5205889 IC50 = 22.4 nM 7.65
CHEMBL5208265 IC50 = 24.4 nM 7.61
CHEMBL5193597 IC50 = 28.0 nM 7.55
CHEMBL5175574 IC50 = 30.7 nM 7.51
CHEMBL5170025 IC50 = 38.1 nM 7.42
CHEMBL4072833 EVOBRUTINIB IC50 = 56.2 nM 7.25
CHEMBL5206496 IC50 = 84.1 nM 7.08
CHEMBL5206093 IC50 = 319.8 nM 6.50
CHEMBL5206716 IC50 = 454.5 nM 6.34
CHEMBL5171858 IC50 = 2526.0 nM 5.60