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Assay Detail

CHEMBL4414893

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

Binding
Inhibition of BTK in human Ramos cells assessed as reduction in BTK phosphorylation at Tyr223 residue preincubated for 1 hr followed by pervanadate or Na3VO4 stimulation for 20 mins by HTRF assay
ChEMBL ↗
49
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Ramos
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 8.21 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3925102 — — 1 9.10
CHEMBL4447328 — — 1 9.00
CHEMBL3962133 — — 1 8.82
CHEMBL3922120 — — 1 8.82
CHEMBL3965549 — — 3 8.80
CHEMBL3936761 ZANUBRUTINIB 4.0 1 8.74
CHEMBL3921167 — — 3 8.70
CHEMBL3908905 — — 1 8.60
CHEMBL3926191 — — 3 8.60
CHEMBL3917026 — — 3 8.60
CHEMBL3948065 — — 1 8.55
CHEMBL3917732 — — 3 8.52
CHEMBL1873475 IBRUTINIB 4.0 1 8.46
CHEMBL3965262 — — 1 8.41
CHEMBL3910697 — — 3 8.38
CHEMBL3977729 — — 3 8.28
CHEMBL3973566 — — 1 8.19
CHEMBL3924160 — — 1 8.10
CHEMBL3913116 — — 1 8.09
CHEMBL3890068 — — 1 7.78
CHEMBL3944698 — — 1 7.72
CHEMBL3904488 — — 1 7.58
CHEMBL3979176 — — 1 7.36
CHEMBL3897911 — — 1 6.63
CHEMBL3977187 — — 1 6.49
CHEMBL3916800 — — 1 -
CHEMBL3954175 — — 1 -
CHEMBL3935234 — — 1 -
CHEMBL4107402 — — 1 -
CHEMBL3968222 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3925102 — IC50 = 0.8 nM 9.10
CHEMBL4447328 — IC50 = 1.0 nM 9.00
CHEMBL3922120 — IC50 = 1.5 nM 8.82
CHEMBL3962133 — IC50 = 1.5 nM 8.82
CHEMBL3965549 — IC50 = 1.6 nM 8.80
CHEMBL3936761 ZANUBRUTINIB IC50 = 1.8 nM 8.74
CHEMBL3921167 — IC50 = 2.0 nM 8.70
CHEMBL3908905 — IC50 = 2.5 nM 8.60
CHEMBL3926191 — IC50 = 2.5 nM 8.60
CHEMBL3917026 — IC50 = 2.5 nM 8.60
CHEMBL3948065 — IC50 = 2.8 nM 8.55
CHEMBL3917732 — IC50 = 3.0 nM 8.52
CHEMBL1873475 IBRUTINIB IC50 = 3.5 nM 8.46
CHEMBL3965262 — IC50 = 3.9 nM 8.41
CHEMBL3965549 — IC50 = 4.2 nM 8.38
CHEMBL3910697 — IC50 = 4.2 nM 8.38
CHEMBL3977729 — IC50 = 5.3 nM 8.28
CHEMBL3973566 — IC50 = 6.4 nM 8.19
CHEMBL3924160 — IC50 = 8.0 nM 8.10
CHEMBL3913116 — IC50 = 8.2 nM 8.09
CHEMBL3921167 — IC50 = 8.7 nM 8.06
CHEMBL3890068 — IC50 = 16.7 nM 7.78
CHEMBL3944698 — IC50 = 18.9 nM 7.72
CHEMBL3904488 — IC50 = 26.3 nM 7.58
CHEMBL3979176 — IC50 = 43.4 nM 7.36
CHEMBL3977729 — IC50 = 63.3 nM 7.20
CHEMBL3897911 — IC50 = 232.6 nM 6.63
CHEMBL3977187 — IC50 = 322.2 nM 6.49
CHEMBL3906546 — IC50 - — -
CHEMBL3926191 — IC50 - — -
CHEMBL3954175 — IC50 - — -
CHEMBL3910697 — IC50 - — -
CHEMBL3917026 — IC50 - — -
CHEMBL3910697 — IC50 - — -
CHEMBL3917026 — IC50 - — -
CHEMBL3973435 — IC50 - — -
CHEMBL3968222 — IC50 < 0.5 nM -
CHEMBL3926191 — IC50 - — -
CHEMBL3965549 — IC50 - — -
CHEMBL3935234 — IC50 - — -
CHEMBL3917732 — IC50 - — -
CHEMBL3977729 — IC50 - — -
CHEMBL3917732 — IC50 - — -
CHEMBL3906908 — IC50 - — -
CHEMBL3921167 — IC50 - — -
CHEMBL3916800 — IC50 - — -
CHEMBL3921373 — IC50 - — -
CHEMBL3926815 — IC50 - — -
CHEMBL4107402 — IC50 - — -