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Assay Detail

CHEMBL3136683

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

Binding
Inhibition of His-tagged L3MBTL1 (unknown origin) using H4K20Me1 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay
25
Total Activities
25
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

Lethal(3)malignant brain tumor-like protein 1 (CHEMBL1287622)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
Camerino MA, Zhong N, Dong A, Dickson BM, James LI, Baughman BM, Norris JL, Kireev DB, Janzen WP, Arrowsmith CH, Frye SV.
Medchemcomm (2013) 4 : 1501 -1507
PubMed 24466405 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 4.40 5.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2426364 1 5.05
CHEMBL3134134 1 5.00
CHEMBL3134131 1 4.85
CHEMBL1235119 1 4.68
CHEMBL3134130 1 4.68
CHEMBL3134135 1 4.52
CHEMBL3134140 1 4.50
CHEMBL3134143 1 4.36
CHEMBL3134136 1 4.35
CHEMBL3134132 1 4.30
CHEMBL3134126 1 4.30
CHEMBL3134137 1 4.29
CHEMBL3134133 1 4.24
CHEMBL3134146 1 4.22
CHEMBL3134125 1 4.20
CHEMBL3134129 1 4.19
CHEMBL3134144 1 4.07
CHEMBL3134139 1 4.06
CHEMBL3134141 1 4.05
CHEMBL3134128 1 4.04
CHEMBL3134138 1 -
CHEMBL3134142 1 -
CHEMBL3134127 1 -
CHEMBL2426474 1 -
CHEMBL3134145 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2426364 IC50 = 8900.0 nM 5.05
CHEMBL3134134 IC50 = 10000.0 nM 5.00
CHEMBL3134131 IC50 = 14000.0 nM 4.85
CHEMBL1235119 IC50 = 21000.0 nM 4.68
CHEMBL3134130 IC50 = 21000.0 nM 4.68
CHEMBL3134135 IC50 = 30000.0 nM 4.52
CHEMBL3134140 IC50 = 32000.0 nM 4.50
CHEMBL3134143 IC50 = 44000.0 nM 4.36
CHEMBL3134136 IC50 = 45000.0 nM 4.35
CHEMBL3134132 IC50 = 50000.0 nM 4.30
CHEMBL3134126 IC50 = 50000.0 nM 4.30
CHEMBL3134137 IC50 = 51000.0 nM 4.29
CHEMBL3134133 IC50 = 57000.0 nM 4.24
CHEMBL3134146 IC50 = 60000.0 nM 4.22
CHEMBL3134125 IC50 = 63000.0 nM 4.20
CHEMBL3134129 IC50 = 65000.0 nM 4.19
CHEMBL3134144 IC50 = 86000.0 nM 4.07
CHEMBL3134139 IC50 = 88000.0 nM 4.06
CHEMBL3134141 IC50 = 90000.0 nM 4.05
CHEMBL3134128 IC50 = 92000.0 nM 4.04
CHEMBL3134138 IC50 > 300000.0 nM -
CHEMBL3134142 IC50 = 128000.0 nM -
CHEMBL3134127 IC50 = 125000.0 nM -
CHEMBL2426474 IC50 = 170000.0 nM -
CHEMBL3134145 IC50 = 152000.0 nM -