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Assay Detail

CHEMBL4477004

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

Binding
Inhibition of SUV39H2 (unknown origin) using H3 histone peptide substrate and [3H]-SAM incubated for 3 hrs by microbeta counting based assay
460
Total Activities
460
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

Histone-lysine N-methyltransferase SUV39H2 (CHEMBL1795177)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Bicyclic compound and use thereof for inhibiting suv39h2
(2018)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 460 7.72 8.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4553838 1 8.75
CHEMBL4587289 1 8.75
CHEMBL4563069 1 8.73
CHEMBL4520078 1 8.71
CHEMBL4551654 1 8.70
CHEMBL4556599 1 8.68
CHEMBL4556449 1 8.66
CHEMBL4457187 1 8.57
CHEMBL4534136 1 8.54
CHEMBL4551056 1 8.52
CHEMBL4547529 1 8.51
CHEMBL4589569 1 8.48
CHEMBL4558804 1 8.48
CHEMBL4514527 1 8.47
CHEMBL4536861 1 8.46
CHEMBL4569911 1 8.46
CHEMBL4557178 1 8.45
CHEMBL4543316 1 8.43
CHEMBL4532138 1 8.42
CHEMBL4534069 1 8.42
CHEMBL4542129 1 8.40
CHEMBL4513598 1 8.39
CHEMBL4483505 1 8.39
CHEMBL4546702 1 8.38
CHEMBL4531530 1 8.37
CHEMBL4521461 1 8.36
CHEMBL4545245 1 8.36
CHEMBL4540137 1 8.36
CHEMBL4515775 1 8.36
CHEMBL4561226 1 8.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4587289 IC50 = 1.77 nM 8.75
CHEMBL4553838 IC50 = 1.78 nM 8.75
CHEMBL4563069 IC50 = 1.88 nM 8.73
CHEMBL4520078 IC50 = 1.97 nM 8.71
CHEMBL4551654 IC50 = 2.0 nM 8.70
CHEMBL4556599 IC50 = 2.07 nM 8.68
CHEMBL4556449 IC50 = 2.2 nM 8.66
CHEMBL4457187 IC50 = 2.71 nM 8.57
CHEMBL4534136 IC50 = 2.9 nM 8.54
CHEMBL4551056 IC50 = 3.0 nM 8.52
CHEMBL4547529 IC50 = 3.1 nM 8.51
CHEMBL4558804 IC50 = 3.33 nM 8.48
CHEMBL4589569 IC50 = 3.27 nM 8.48
CHEMBL4514527 IC50 = 3.35 nM 8.47
CHEMBL4569911 IC50 = 3.49 nM 8.46
CHEMBL4536861 IC50 = 3.5 nM 8.46
CHEMBL4557178 IC50 = 3.53 nM 8.45
CHEMBL4543316 IC50 = 3.71 nM 8.43
CHEMBL4534069 IC50 = 3.81 nM 8.42
CHEMBL4532138 IC50 = 3.81 nM 8.42
CHEMBL4542129 IC50 = 3.95 nM 8.40
CHEMBL4483505 IC50 = 4.03 nM 8.39
CHEMBL4513598 IC50 = 4.11 nM 8.39
CHEMBL4546702 IC50 = 4.16 nM 8.38
CHEMBL4531530 IC50 = 4.31 nM 8.37
CHEMBL4540137 IC50 = 4.33 nM 8.36
CHEMBL4521461 IC50 = 4.35 nM 8.36
CHEMBL4545245 IC50 = 4.4 nM 8.36
CHEMBL4515775 IC50 = 4.35 nM 8.36
CHEMBL4561226 IC50 = 4.54 nM 8.34
CHEMBL4585867 IC50 = 4.94 nM 8.31
CHEMBL4580507 IC50 = 4.88 nM 8.31
CHEMBL4574141 IC50 = 4.89 nM 8.31
CHEMBL4576486 IC50 = 5.05 nM 8.30
CHEMBL4575122 IC50 = 4.99 nM 8.30
CHEMBL4586982 IC50 = 5.15 nM 8.29
CHEMBL4573226 IC50 = 5.14 nM 8.29
CHEMBL4561677 IC50 = 5.24 nM 8.28
CHEMBL4543399 IC50 = 5.31 nM 8.28
CHEMBL4554934 IC50 = 5.38 nM 8.27
CHEMBL4591003 IC50 = 5.4 nM 8.27
CHEMBL4528102 IC50 = 5.44 nM 8.26
CHEMBL4582832 IC50 = 5.61 nM 8.25
CHEMBL4557490 IC50 = 5.75 nM 8.24
CHEMBL4513575 IC50 = 5.74 nM 8.24
CHEMBL4515431 IC50 = 5.85 nM 8.23
CHEMBL4553698 IC50 = 6.08 nM 8.22
CHEMBL4593564 IC50 = 6.05 nM 8.22
CHEMBL4530406 IC50 = 5.97 nM 8.22
CHEMBL4516650 IC50 = 6.06 nM 8.22