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Assay Detail

CHEMBL4414894

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

Binding
Inhibition of N-terminal His-tagged recombinant human BTK (393 to 659 residues) expressed in baculovirus infected Sf9 cells preincubated for 1 hr followed by Biotin-AVLESEEELYSSARQ-NH2 substrate addition in presence of ATP and measured after 1 hr by TR-FRET assay
ChEMBL ↗
49
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase BTK (CHEMBL5251) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
Guo Y, Liu Y, Hu N, Yu D, Zhou C, Shi G, Zhang B, Wei M, Liu J, Luo L, Tang Z, Song H, Guo Y, Liu X, Su D, Zhang S, Song X, Zhou X, Hong Y, Chen S, Cheng Z, Young S, Wei Q, Wang H, Wang Q, Lv L, Wang F, Xu H, Sun H, Xing H, Li N, Zhang W, Wang Z, Liu G, Sun Z, Zhou D, Li W, Liu L, Wang L, Wang Z.
J Med Chem (2019) 62 : 7923 -7940
PubMed 31381333 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 8.46 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3925102 — — 1 9.89
CHEMBL3962133 — — 1 9.89
CHEMBL3968222 — — 1 9.85
CHEMBL3922120 — — 1 9.82
CHEMBL3973566 — — 1 9.72
CHEMBL3977729 — — 3 9.62
CHEMBL3936761 ZANUBRUTINIB 4.0 1 9.52
CHEMBL3948065 — — 1 9.49
CHEMBL3913116 — — 1 9.44
CHEMBL3917732 — — 3 9.42
CHEMBL3965549 — — 3 9.28
CHEMBL3973435 — — 1 9.20
CHEMBL3910697 — — 3 9.19
CHEMBL3926191 — — 3 9.00
CHEMBL3917026 — — 3 8.92
CHEMBL3904488 — — 1 8.89
CHEMBL3965262 — — 1 8.80
CHEMBL3908905 — — 1 8.72
CHEMBL3921167 — — 3 8.66
CHEMBL3890068 — — 1 8.57
CHEMBL3924160 — — 1 8.57
CHEMBL3944698 — — 1 8.46
CHEMBL3906546 — — 1 8.38
CHEMBL3954175 — — 1 8.38
CHEMBL3897911 — — 1 8.33
CHEMBL3979176 — — 1 8.02
CHEMBL4107402 — — 1 7.96
CHEMBL3935234 — — 1 7.85
CHEMBL3977187 — — 1 7.77
CHEMBL3926815 — — 1 7.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3925102 — IC50 = 0.13 nM 9.89
CHEMBL3962133 — IC50 = 0.13 nM 9.89
CHEMBL3968222 — IC50 = 0.14 nM 9.85
CHEMBL3922120 — IC50 = 0.15 nM 9.82
CHEMBL3973566 — IC50 = 0.19 nM 9.72
CHEMBL3977729 — IC50 = 0.24 nM 9.62
CHEMBL3936761 ZANUBRUTINIB IC50 = 0.3 nM 9.52
CHEMBL3948065 — IC50 = 0.32 nM 9.49
CHEMBL3913116 — IC50 = 0.36 nM 9.44
CHEMBL3917732 — IC50 = 0.38 nM 9.42
CHEMBL3965549 — IC50 = 0.53 nM 9.28
CHEMBL3965549 — IC50 = 0.58 nM 9.24
CHEMBL3917732 — IC50 = 0.62 nM 9.21
CHEMBL3973435 — IC50 = 0.63 nM 9.20
CHEMBL3910697 — IC50 = 0.64 nM 9.19
CHEMBL3910697 — IC50 = 0.78 nM 9.11
CHEMBL3977729 — IC50 = 0.9 nM 9.05
CHEMBL3926191 — IC50 = 1.0 nM 9.00
CHEMBL3917026 — IC50 = 1.2 nM 8.92
CHEMBL3965549 — IC50 = 1.3 nM 8.89
CHEMBL3904488 — IC50 = 1.3 nM 8.89
CHEMBL3917026 — IC50 = 1.6 nM 8.80
CHEMBL3965262 — IC50 = 1.6 nM 8.80
CHEMBL3926191 — IC50 = 1.9 nM 8.72
CHEMBL3908905 — IC50 = 1.9 nM 8.72
CHEMBL3921167 — IC50 = 2.2 nM 8.66
CHEMBL3921167 — IC50 = 2.6 nM 8.59
CHEMBL3924160 — IC50 = 2.7 nM 8.57
CHEMBL3890068 — IC50 = 2.7 nM 8.57
CHEMBL3921167 — IC50 = 2.7 nM 8.57
CHEMBL3944698 — IC50 = 3.5 nM 8.46
CHEMBL3954175 — IC50 = 4.2 nM 8.38
CHEMBL3906546 — IC50 = 4.2 nM 8.38
CHEMBL3897911 — IC50 = 4.7 nM 8.33
CHEMBL3979176 — IC50 = 9.5 nM 8.02
CHEMBL3977729 — IC50 = 11.0 nM 7.96
CHEMBL4107402 — IC50 = 11.0 nM 7.96
CHEMBL3935234 — IC50 = 14.0 nM 7.85
CHEMBL3977187 — IC50 = 17.0 nM 7.77
CHEMBL3926815 — IC50 = 34.0 nM 7.47
CHEMBL3916800 — IC50 = 41.0 nM 7.39
CHEMBL3917026 — IC50 = 120.0 nM 6.92
CHEMBL3926191 — IC50 = 130.0 nM 6.89
CHEMBL3917732 — IC50 = 130.0 nM 6.89
CHEMBL3906908 — IC50 = 150.0 nM 6.82
CHEMBL3949083 — IC50 = 200.0 nM 6.70
CHEMBL3921373 — IC50 = 860.0 nM 6.07
CHEMBL3969103 — IC50 = 1000.0 nM 6.00
CHEMBL3910697 — IC50 = 1500.0 nM 5.82