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Assay Detail

CHEMBL5106226

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

Binding
Inhibition of BTK (unknown origin) measured by ADP-Glo assay
ChEMBL ↗
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tyrosine-protein kinase BTK (CHEMBL5251) ↗
Type SINGLE PROTEIN
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 49 8.34 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1873475 IBRUTINIB 4.0 1 9.70
CHEMBL5180302 — — 1 9.40
CHEMBL5195504 — — 1 9.30
CHEMBL5192748 — — 1 9.30
CHEMBL5208265 — — 1 9.22
CHEMBL5206496 — — 1 9.15
CHEMBL5193942 — — 1 9.15
CHEMBL5170025 — — 1 9.10
CHEMBL5204458 — — 1 9.10
CHEMBL5176551 — — 1 9.10
CHEMBL5196932 — — 1 9.10
CHEMBL5177044 — — 1 9.10
CHEMBL5198455 — — 1 9.00
CHEMBL5170833 — — 1 8.96
CHEMBL5189426 — — 1 8.92
CHEMBL5189231 — — 1 8.92
CHEMBL5178389 — — 1 8.89
CHEMBL5196670 — — 1 8.87
CHEMBL5202754 — — 1 8.85
CHEMBL5179204 — — 1 8.85
CHEMBL5193597 — — 1 8.85
CHEMBL5205889 — — 1 8.80
CHEMBL4072833 EVOBRUTINIB 3.0 1 8.74
CHEMBL5179080 — — 1 8.72
CHEMBL5206716 — — 1 8.72
CHEMBL5193930 — — 1 8.72
CHEMBL5175574 — — 1 8.70
CHEMBL5187153 — — 1 8.68
CHEMBL5206497 — — 1 8.66
CHEMBL5206093 — — 1 8.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1873475 IBRUTINIB IC50 = 0.2 nM 9.70
CHEMBL5180302 — IC50 = 0.4 nM 9.40
CHEMBL5192748 — IC50 = 0.5 nM 9.30
CHEMBL5195504 — IC50 = 0.5 nM 9.30
CHEMBL5208265 — IC50 = 0.6 nM 9.22
CHEMBL5206496 — IC50 = 0.7 nM 9.15
CHEMBL5193942 — IC50 = 0.7 nM 9.15
CHEMBL5170025 — IC50 = 0.8 nM 9.10
CHEMBL5204458 — IC50 = 0.8 nM 9.10
CHEMBL5176551 — IC50 = 0.8 nM 9.10
CHEMBL5196932 — IC50 = 0.8 nM 9.10
CHEMBL5177044 — IC50 = 0.8 nM 9.10
CHEMBL5198455 — IC50 = 1.0 nM 9.00
CHEMBL5170833 — IC50 = 1.1 nM 8.96
CHEMBL5189231 — IC50 = 1.2 nM 8.92
CHEMBL5189426 — IC50 = 1.2 nM 8.92
CHEMBL5178389 — IC50 = 1.3 nM 8.89
CHEMBL5196670 — IC50 = 1.34 nM 8.87
CHEMBL5202754 — IC50 = 1.4 nM 8.85
CHEMBL5179204 — IC50 = 1.4 nM 8.85
CHEMBL5193597 — IC50 = 1.4 nM 8.85
CHEMBL5205889 — IC50 = 1.6 nM 8.80
CHEMBL4072833 EVOBRUTINIB IC50 = 1.83 nM 8.74
CHEMBL5193930 — IC50 = 1.9 nM 8.72
CHEMBL5206716 — IC50 = 1.9 nM 8.72
CHEMBL5179080 — IC50 = 1.9 nM 8.72
CHEMBL5175574 — IC50 = 2.0 nM 8.70
CHEMBL5187153 — IC50 = 2.1 nM 8.68
CHEMBL5206497 — IC50 = 2.2 nM 8.66
CHEMBL5206093 — IC50 = 2.2 nM 8.66
CHEMBL5188524 — IC50 = 2.5 nM 8.60
CHEMBL5171858 — IC50 = 4.5 nM 8.35
CHEMBL5203573 — IC50 = 8.4 nM 8.08
CHEMBL5179333 — IC50 = 11.1 nM 7.96
CHEMBL5208592 — IC50 = 16.4 nM 7.79
CHEMBL5179757 — IC50 = 17.3 nM 7.76
CHEMBL5184628 — IC50 = 23.2 nM 7.63
CHEMBL5183474 — IC50 = 26.2 nM 7.58
CHEMBL3647420 PYROTINIB IC50 = 31.7 nM 7.50
CHEMBL5191643 — IC50 = 52.3 nM 7.28
CHEMBL5206968 — IC50 = 68.5 nM 7.16
CHEMBL5197246 — IC50 = 92.9 nM 7.03
CHEMBL3701238 FUTIBATINIB IC50 = 94.9 nM 7.02
CHEMBL5184198 — IC50 = 98.7 nM 7.01
CHEMBL5187334 — IC50 = 153.3 nM 6.81
CHEMBL5188432 — IC50 = 593.1 nM 6.23
CHEMBL5198805 — IC50 = 973.8 nM 6.01
CHEMBL5191588 — IC50 = 5410.2 nM 5.27
CHEMBL5179004 — IC50 > 10000.0 nM -