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Assay Detail

CHEMBL2429080

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

Binding
Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay
ChEMBL ↗
56
Total Activities
56
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 3 (CHEMBL1287623) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.
James LI, Korboukh VK, Krichevsky L, Baughman BM, Herold JM, Norris JL, Jin J, Kireev DB, Janzen WP, Arrowsmith CH, Frye SV.
J Med Chem (2013) 56 : 7358 -7371
PubMed 24040942 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 56 6.58 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2426360 — — 1 7.37
CHEMBL2426498 — — 1 7.32
CHEMBL2426364 — — 1 7.31
CHEMBL2426365 — — 1 7.30
CHEMBL2426366 — — 1 7.29
CHEMBL2426367 — — 1 7.28
CHEMBL2424678 — — 1 7.21
CHEMBL2426368 — — 1 7.21
CHEMBL2426363 — — 1 7.17
CHEMBL2426476 — — 1 7.13
CHEMBL2426496 — — 1 7.13
CHEMBL2426489 — — 1 7.09
CHEMBL2426477 — — 1 7.06
CHEMBL2426495 — — 1 7.04
CHEMBL2426490 — — 1 7.04
CHEMBL2426481 — — 1 7.01
CHEMBL2426480 — — 1 6.96
CHEMBL2426469 — — 1 6.96
CHEMBL2426358 — — 1 6.89
CHEMBL2426483 — — 1 6.89
CHEMBL2424677 — — 1 6.85
CHEMBL2426482 — — 1 6.82
CHEMBL2426374 — — 1 6.82
CHEMBL2426376 — — 1 6.80
CHEMBL2426375 — — 1 6.80
CHEMBL2426484 — — 1 6.80
CHEMBL2426488 — — 1 6.75
CHEMBL2426485 — — 1 6.68
CHEMBL2426478 — — 1 6.66
CHEMBL2426462 — — 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2426360 — IC50 = 43.0 nM 7.37
CHEMBL2426498 — IC50 = 48.0 nM 7.32
CHEMBL2426364 — IC50 = 49.0 nM 7.31
CHEMBL2426365 — IC50 = 50.0 nM 7.30
CHEMBL2426366 — IC50 = 51.0 nM 7.29
CHEMBL2426367 — IC50 = 53.0 nM 7.28
CHEMBL2424678 — IC50 = 61.0 nM 7.21
CHEMBL2426368 — IC50 = 61.0 nM 7.21
CHEMBL2426363 — IC50 = 68.0 nM 7.17
CHEMBL2426476 — IC50 = 74.0 nM 7.13
CHEMBL2426496 — IC50 = 74.0 nM 7.13
CHEMBL2426489 — IC50 = 81.0 nM 7.09
CHEMBL2426477 — IC50 = 88.0 nM 7.06
CHEMBL2426495 — IC50 = 92.0 nM 7.04
CHEMBL2426490 — IC50 = 92.0 nM 7.04
CHEMBL2426481 — IC50 = 97.0 nM 7.01
CHEMBL2426480 — IC50 = 110.0 nM 6.96
CHEMBL2426469 — IC50 = 110.0 nM 6.96
CHEMBL2426358 — IC50 = 130.0 nM 6.89
CHEMBL2426483 — IC50 = 130.0 nM 6.89
CHEMBL2424677 — IC50 = 140.0 nM 6.85
CHEMBL2426482 — IC50 = 150.0 nM 6.82
CHEMBL2426374 — IC50 = 150.0 nM 6.82
CHEMBL2426484 — IC50 = 160.0 nM 6.80
CHEMBL2426376 — IC50 = 160.0 nM 6.80
CHEMBL2426375 — IC50 = 160.0 nM 6.80
CHEMBL2426488 — IC50 = 180.0 nM 6.75
CHEMBL2426485 — IC50 = 210.0 nM 6.68
CHEMBL2426478 — IC50 = 220.0 nM 6.66
CHEMBL2426462 — IC50 = 220.0 nM 6.66
CHEMBL2426359 — IC50 = 240.0 nM 6.62
CHEMBL2426494 — IC50 = 250.0 nM 6.60
CHEMBL2426470 — IC50 = 280.0 nM 6.55
CHEMBL2426497 — IC50 = 290.0 nM 6.54
CHEMBL2426461 — IC50 = 300.0 nM 6.52
CHEMBL2426362 — IC50 = 310.0 nM 6.51
CHEMBL2426463 — IC50 = 340.0 nM 6.47
CHEMBL2426479 — IC50 = 350.0 nM 6.46
CHEMBL2426373 — IC50 = 350.0 nM 6.46
CHEMBL2426471 — IC50 = 350.0 nM 6.46
CHEMBL2426361 — IC50 = 450.0 nM 6.35
CHEMBL2426466 — IC50 = 620.0 nM 6.21
CHEMBL2426493 — IC50 = 770.0 nM 6.11
CHEMBL2426491 — IC50 = 800.0 nM 6.10
CHEMBL2426472 — IC50 = 800.0 nM 6.10
CHEMBL2426486 — IC50 = 1100.0 nM 5.96
CHEMBL2426487 — IC50 = 1600.0 nM 5.80
CHEMBL2426473 — IC50 = 1900.0 nM 5.72
CHEMBL2426465 — IC50 = 2200.0 nM 5.66
CHEMBL2426464 — IC50 = 2700.0 nM 5.57