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Assay Detail

CHEMBL4414895

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

ADMET
Inhibition of EGFR (unknown origin) 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 ↗
48
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Epidermal growth factor receptor (CHEMBL203) ↗
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 48 8.33 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3910697 — — 3 9.74
CHEMBL3917026 — — 3 9.52
CHEMBL3965262 — — 1 9.47
CHEMBL3906546 — — 1 9.34
CHEMBL3926191 — — 3 9.32
CHEMBL3890068 — — 1 9.20
CHEMBL3954175 — — 1 9.18
CHEMBL3977729 — — 3 9.14
CHEMBL1873475 IBRUTINIB 4.0 1 9.12
CHEMBL3904488 — — 1 9.10
CHEMBL3908905 — — 1 8.92
CHEMBL3965549 — — 3 8.68
CHEMBL3948065 — — 1 8.66
CHEMBL3936761 ZANUBRUTINIB 4.0 1 8.59
CHEMBL3897911 — — 1 8.51
CHEMBL3944698 — — 1 8.49
CHEMBL3977187 — — 1 8.23
CHEMBL3921167 — — 3 6.85
CHEMBL3979176 — — 1 6.77
CHEMBL3924160 — — 1 6.68
CHEMBL3962133 — — 1 -
CHEMBL3916800 — — 1 -
CHEMBL3935234 — — 1 -
CHEMBL4107402 — — 1 -
CHEMBL3973435 — — 1 -
CHEMBL3968222 — — 1 -
CHEMBL3973566 — — 1 -
CHEMBL3926815 — — 1 -
CHEMBL3913116 — — 1 -
CHEMBL3922120 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3910697 — IC50 = 0.18 nM 9.74
CHEMBL3917026 — IC50 = 0.3 nM 9.52
CHEMBL3965262 — IC50 = 0.34 nM 9.47
CHEMBL3906546 — IC50 = 0.46 nM 9.34
CHEMBL3926191 — IC50 = 0.48 nM 9.32
CHEMBL3890068 — IC50 = 0.63 nM 9.20
CHEMBL3954175 — IC50 = 0.66 nM 9.18
CHEMBL3977729 — IC50 = 0.72 nM 9.14
CHEMBL1873475 IBRUTINIB IC50 = 0.75 nM 9.12
CHEMBL3904488 — IC50 = 0.79 nM 9.10
CHEMBL3908905 — IC50 = 1.2 nM 8.92
CHEMBL3965549 — IC50 = 2.1 nM 8.68
CHEMBL3948065 — IC50 = 2.2 nM 8.66
CHEMBL3936761 ZANUBRUTINIB IC50 = 2.6 nM 8.59
CHEMBL3897911 — IC50 = 3.1 nM 8.51
CHEMBL3944698 — IC50 = 3.2 nM 8.49
CHEMBL3977187 — IC50 = 5.9 nM 8.23
CHEMBL3977729 — IC50 = 21.0 nM 7.68
CHEMBL3965549 — IC50 = 27.0 nM 7.57
CHEMBL3926191 — IC50 = 99.0 nM 7.00
CHEMBL3921167 — IC50 = 141.0 nM 6.85
CHEMBL3979176 — IC50 = 169.0 nM 6.77
CHEMBL3924160 — IC50 = 208.0 nM 6.68
CHEMBL3921167 — IC50 = 334.0 nM 6.48
CHEMBL3910697 — IC50 = 1059.0 nM 5.97
CHEMBL3973566 — IC50 < 0.25 nM -
CHEMBL3917026 — IC50 - — -
CHEMBL3925102 — IC50 < 0.25 nM -
CHEMBL3917026 — IC50 - — -
CHEMBL3926815 — IC50 - — -
CHEMBL3926191 — IC50 - — -
CHEMBL3906908 — IC50 - — -
CHEMBL3917732 — IC50 - — -
CHEMBL3922120 — IC50 < 0.25 nM -
CHEMBL3913116 — IC50 < 0.25 nM -
CHEMBL3910697 — IC50 - — -
CHEMBL3962133 — IC50 < 0.25 nM -
CHEMBL3921167 — IC50 - — -
CHEMBL3973435 — IC50 - — -
CHEMBL3917732 — IC50 < 0.25 nM -
CHEMBL4107402 — IC50 - — -
CHEMBL3965549 — IC50 - — -
CHEMBL3968222 — IC50 < 0.25 nM -
CHEMBL3917732 — IC50 - — -
CHEMBL3977729 — IC50 - — -
CHEMBL3935234 — IC50 - — -
CHEMBL3916800 — IC50 - — -
CHEMBL3921373 — IC50 - — -