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Assay Detail

CHEMBL4052448

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

Binding
Binding affinity to human N-terminal MDMx (1 to 134 residues) expressed in Escherichia coli BL21 (DE3) after 15 mins in presence of 5-FAM-LTFEHYWAQLTS by FP assay
29
Total Activities
29
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

Protein Mdm4 (CHEMBL1255126)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers.
Twarda-Clapa A, Krzanik S, Kubica K, Guzik K, Labuzek B, Neochoritis CG, Khoury K, Kowalska K, Czub M, Dubin G, Dömling A, Skalniak L, Holak TA.
J Med Chem (2017) 60 : 4234 -4244
PubMed 28482147 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 4.95 5.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4078749 1 5.50
CHEMBL4067165 1 5.38
CHEMBL4089364 1 5.36
CHEMBL4096099 1 5.33
CHEMBL4098976 1 5.31
CHEMBL4104786 1 5.17
CHEMBL4085272 1 5.01
CHEMBL4104110 1 4.91
CHEMBL4072678 1 4.83
CHEMBL4093959 1 4.58
CHEMBL4094325 1 4.56
CHEMBL4099580 1 4.53
CHEMBL4084081 1 4.45
CHEMBL4077617 1 4.40
CHEMBL4096776 1 -
CHEMBL4064085 1 -
CHEMBL4091842 1 -
CHEMBL4102063 1 -
CHEMBL4073720 1 -
CHEMBL4060276 1 -
CHEMBL4088498 1 -
CHEMBL4081423 1 -
CHEMBL4086204 1 -
CHEMBL4066410 1 -
CHEMBL4075565 1 -
CHEMBL4068179 1 -
CHEMBL4063649 1 -
CHEMBL4071052 1 -
CHEMBL4086907 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4078749 Ki = 3150.0 nM 5.50
CHEMBL4067165 Ki = 4170.0 nM 5.38
CHEMBL4089364 Ki = 4400.0 nM 5.36
CHEMBL4096099 Ki = 4710.0 nM 5.33
CHEMBL4098976 Ki = 4910.0 nM 5.31
CHEMBL4104786 Ki = 6760.0 nM 5.17
CHEMBL4085272 Ki = 9750.0 nM 5.01
CHEMBL4104110 Ki = 12400.0 nM 4.91
CHEMBL4072678 Ki = 14700.0 nM 4.83
CHEMBL4093959 Ki = 26300.0 nM 4.58
CHEMBL4094325 Ki = 27400.0 nM 4.56
CHEMBL4099580 Ki = 29600.0 nM 4.53
CHEMBL4084081 Ki = 35300.0 nM 4.45
CHEMBL4077617 Ki = 40200.0 nM 4.40
CHEMBL4096776 Ki - -
CHEMBL4064085 Ki - -
CHEMBL4091842 Ki - -
CHEMBL4102063 Ki - -
CHEMBL4073720 Ki - -
CHEMBL4060276 Ki - -
CHEMBL4088498 Ki - -
CHEMBL4081423 Ki - -
CHEMBL4086204 Ki - -
CHEMBL4066410 Ki - -
CHEMBL4075565 Ki - -
CHEMBL4068179 Ki - -
CHEMBL4063649 Ki - -
CHEMBL4071052 Ki - -
CHEMBL4086907 Ki - -