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Assay Detail

CHEMBL4366888

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Binding
Inhibition of FAM-probe binding to Menin (unknown origin) after 60 mins by fluorescence polarization competitive binding assay
ChEMBL ↗
76
Total Activities
38
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Menin (CHEMBL1615381) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Discovery of M-89 as a Highly Potent Inhibitor of the Menin-Mixed Lineage Leukemia (Menin-MLL) Protein-Protein Interaction.
Aguilar A, Zheng K, Xu T, Xu S, Huang L, Fernandez-Salas E, Liu L, Bernard D, Harvey KP, Foster C, McEachern D, Stuckey J, Chinnaswamy K, Delproposto J, Kampf JW, Wang S.
J Med Chem (2019) 62 : 6015 -6034
PubMed 31244110 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 6.97 8.30
Ki 38 7.50 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4585198 — — 2 9.00
CHEMBL4592636 — — 2 8.85
CHEMBL4551865 — — 2 8.85
CHEMBL4449199 — — 2 8.77
CHEMBL4522767 — — 2 8.70
CHEMBL4516680 — — 2 8.70
CHEMBL4578509 — — 2 8.62
CHEMBL4458829 — — 2 8.57
CHEMBL4444304 — — 2 8.57
CHEMBL4476073 — — 2 8.34
CHEMBL4459554 — — 2 8.34
CHEMBL4449381 — — 2 8.30
CHEMBL4436641 — — 2 8.25
CHEMBL4470192 — — 2 8.15
CHEMBL4532417 — — 2 8.15
CHEMBL4568235 — — 2 8.07
CHEMBL4452253 — — 2 8.01
CHEMBL4460234 — — 2 8.00
CHEMBL4446177 — — 2 7.96
CHEMBL4581439 — — 2 7.96
CHEMBL4453006 — — 2 7.92
CHEMBL4467100 — — 2 7.68
CHEMBL4448045 — — 2 7.66
CHEMBL4466955 — — 2 7.57
CHEMBL4565646 — — 2 7.50
CHEMBL4592512 — — 2 7.35
CHEMBL3126196 — — 2 7.24
CHEMBL4537683 — — 2 6.68
CHEMBL4453547 — — 2 6.46
CHEMBL4448156 — — 2 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4585198 — Ki = 1.0 nM 9.00
CHEMBL4592636 — Ki = 1.4 nM 8.85
CHEMBL4551865 — Ki = 1.4 nM 8.85
CHEMBL4449199 — Ki = 1.7 nM 8.77
CHEMBL4522767 — Ki = 2.0 nM 8.70
CHEMBL4516680 — Ki = 2.0 nM 8.70
CHEMBL4578509 — Ki = 2.4 nM 8.62
CHEMBL4458829 — Ki = 2.7 nM 8.57
CHEMBL4444304 — Ki = 2.7 nM 8.57
CHEMBL4459554 — Ki = 4.6 nM 8.34
CHEMBL4476073 — Ki = 4.6 nM 8.34
CHEMBL4449381 — IC50 = 5.0 nM 8.30
CHEMBL4436641 — Ki = 5.6 nM 8.25
CHEMBL4585198 — IC50 = 6.0 nM 8.22
CHEMBL4470192 — Ki = 7.0 nM 8.15
CHEMBL4551865 — IC50 = 7.0 nM 8.15
CHEMBL4592636 — IC50 = 7.0 nM 8.15
CHEMBL4532417 — Ki = 7.0 nM 8.15
CHEMBL4449199 — IC50 = 8.0 nM 8.10
CHEMBL4568235 — Ki = 8.5 nM 8.07
CHEMBL4522767 — IC50 = 9.0 nM 8.05
CHEMBL4452253 — Ki = 9.7 nM 8.01
CHEMBL4460234 — Ki = 10.0 nM 8.00
CHEMBL4578509 — IC50 = 10.0 nM 8.00
CHEMBL4446177 — Ki = 11.0 nM 7.96
CHEMBL4581439 — Ki = 11.0 nM 7.96
CHEMBL4444304 — IC50 = 11.0 nM 7.96
CHEMBL4458829 — IC50 = 11.0 nM 7.96
CHEMBL4516680 — IC50 = 11.0 nM 7.96
CHEMBL4453006 — Ki = 12.0 nM 7.92
CHEMBL4476073 — IC50 = 17.0 nM 7.77
CHEMBL4459554 — IC50 = 17.0 nM 7.77
CHEMBL4436641 — IC50 = 20.0 nM 7.70
CHEMBL4467100 — Ki = 21.0 nM 7.68
CHEMBL4448045 — Ki = 22.0 nM 7.66
CHEMBL4470192 — IC50 = 25.0 nM 7.60
CHEMBL4532417 — IC50 = 25.0 nM 7.60
CHEMBL4466955 — Ki = 27.0 nM 7.57
CHEMBL4568235 — IC50 = 29.0 nM 7.54
CHEMBL4565646 — Ki = 32.0 nM 7.50
CHEMBL4452253 — IC50 = 33.0 nM 7.48
CHEMBL4460234 — IC50 = 34.0 nM 7.47
CHEMBL4446177 — IC50 = 36.0 nM 7.44
CHEMBL4581439 — IC50 = 36.0 nM 7.44
CHEMBL4453006 — IC50 = 40.0 nM 7.40
CHEMBL4592512 — Ki = 45.0 nM 7.35
CHEMBL3126196 — Ki = 58.0 nM 7.24
CHEMBL4467100 — IC50 = 67.0 nM 7.17
CHEMBL4448045 — IC50 = 71.0 nM 7.15
CHEMBL4466955 — IC50 = 88.0 nM 7.06