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Assay Detail

CHEMBL5237550

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

Binding
Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay
42
Total Activities
42
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-arginine methyltransferase CARM1 (CHEMBL5406)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Discovery of Potent CARM1 Inhibitors for Solid Tumor and Cancer Immunology Therapy.
Zhang Z, Guo Z, Xu X, Cao D, Yang H, Li Y, Shi Q, Du Z, Guo X, Wang X, Chen D, Zhang Y, Chen L, Zhou K, Li J, Geng M, Huang X, Xiong B.
J Med Chem (2021) 64 : 16650 -16674
PubMed 34781683 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 8.16 9.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5272699 1 9.19
CHEMBL5270700 1 9.11
CHEMBL5274219 1 9.04
CHEMBL5291238 1 8.96
CHEMBL5271782 1 8.95
CHEMBL5288947 1 8.79
CHEMBL5283756 1 8.64
CHEMBL5287824 1 8.61
CHEMBL5271800 1 8.53
CHEMBL5266562 1 8.43
CHEMBL5289496 1 8.43
CHEMBL5284876 1 8.42
CHEMBL5289683 1 8.42
CHEMBL5268692 1 8.37
CHEMBL5274541 1 8.37
CHEMBL5277620 1 8.36
CHEMBL5273938 1 8.29
CHEMBL5279093 1 8.28
CHEMBL5290292 1 8.22
CHEMBL5269937 1 8.21
CHEMBL5289773 1 7.99
CHEMBL5290611 1 7.99
CHEMBL5285757 1 7.94
CHEMBL5266548 1 7.93
CHEMBL5270405 1 7.93
CHEMBL5279447 1 7.88
CHEMBL5271681 1 7.71
CHEMBL5287686 1 7.67
CHEMBL5289833 1 7.66
CHEMBL5266710 1 7.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5272699 IC50 = 0.65 nM 9.19
CHEMBL5270700 IC50 = 0.78 nM 9.11
CHEMBL5274219 IC50 = 0.92 nM 9.04
CHEMBL5291238 IC50 = 1.1 nM 8.96
CHEMBL5271782 IC50 = 1.13 nM 8.95
CHEMBL5288947 IC50 = 1.63 nM 8.79
CHEMBL5283756 IC50 = 2.3 nM 8.64
CHEMBL5287824 IC50 = 2.46 nM 8.61
CHEMBL5271800 IC50 = 2.94 nM 8.53
CHEMBL5266562 IC50 = 3.7 nM 8.43
CHEMBL5289496 IC50 = 3.68 nM 8.43
CHEMBL5284876 IC50 = 3.84 nM 8.42
CHEMBL5289683 IC50 = 3.78 nM 8.42
CHEMBL5268692 IC50 = 4.24 nM 8.37
CHEMBL5274541 IC50 = 4.29 nM 8.37
CHEMBL5277620 IC50 = 4.37 nM 8.36
CHEMBL5273938 IC50 = 5.13 nM 8.29
CHEMBL5279093 IC50 = 5.2 nM 8.28
CHEMBL5290292 IC50 = 6.07 nM 8.22
CHEMBL5269937 IC50 = 6.15 nM 8.21
CHEMBL5290611 IC50 = 10.18 nM 7.99
CHEMBL5289773 IC50 = 10.13 nM 7.99
CHEMBL5285757 IC50 = 11.52 nM 7.94
CHEMBL5266548 IC50 = 11.84 nM 7.93
CHEMBL5270405 IC50 = 11.63 nM 7.93
CHEMBL5279447 IC50 = 13.1 nM 7.88
CHEMBL5271681 IC50 = 19.62 nM 7.71
CHEMBL5287686 IC50 = 21.45 nM 7.67
CHEMBL5289833 IC50 = 21.7 nM 7.66
CHEMBL5266710 IC50 = 26.86 nM 7.57
CHEMBL5278488 IC50 = 29.43 nM 7.53
CHEMBL5279188 IC50 = 29.54 nM 7.53
CHEMBL5288079 IC50 = 31.46 nM 7.50
CHEMBL5277762 IC50 = 33.61 nM 7.47
CHEMBL5290686 IC50 = 60.05 nM 7.22
CHEMBL5267045 IC50 = 187.06 nM 6.73
CHEMBL5288432 IC50 > 1000.0 nM -
CHEMBL5286582 IC50 > 1000.0 nM -
CHEMBL5275579 IC50 > 1000.0 nM -
CHEMBL5266735 IC50 > 1000.0 nM -
CHEMBL5266897 IC50 > 1000.0 nM -
CHEMBL5280681 IC50 > 1000.0 nM -