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Assay Detail

CHEMBL828333

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

Binding
Inhibition of human MTAP as equilibrium dissociation constant
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

S-methyl-5'-thioadenosine phosphorylase (CHEMBL4941)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Second generation transition state analogue inhibitors of human 5'-methylthioadenosine phosphorylase.
Evans GB, Furneaux RH, Lenz DH, Painter GF, Schramm VL, Singh V, Tyler PC.
J Med Chem (2005) 48 : 4679 -4689
PubMed 16000004 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 9.47 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL365813 1 11.00
CHEMBL191544 1 10.47
CHEMBL188375 1 10.05
CHEMBL365378 1 9.96
CHEMBL425188 1 9.92
CHEMBL190216 1 9.80
CHEMBL190139 1 9.80
CHEMBL188034 1 9.77
CHEMBL191281 1 9.59
CHEMBL191177 1 9.57
CHEMBL190867 1 9.43
CHEMBL191436 1 9.15
CHEMBL1161749 1 9.00
CHEMBL189911 1 8.52
CHEMBL189837 1 8.10
CHEMBL189910 1 7.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL365813 Ki = 0.01 nM 11.00
CHEMBL191544 Ki = 0.034 nM 10.47
CHEMBL188375 Ki = 0.09 nM 10.05
CHEMBL365378 Ki = 0.11 nM 9.96
CHEMBL425188 Ki = 0.12 nM 9.92
CHEMBL190216 Ki = 0.16 nM 9.80
CHEMBL190139 Ki = 0.16 nM 9.80
CHEMBL188034 Ki = 0.17 nM 9.77
CHEMBL191281 Ki = 0.26 nM 9.59
CHEMBL191177 Ki = 0.27 nM 9.57
CHEMBL190867 Ki = 0.37 nM 9.43
CHEMBL191436 Ki = 0.7 nM 9.15
CHEMBL1161749 Ki = 1.0 nM 9.00
CHEMBL189911 Ki = 3.0 nM 8.52
CHEMBL189837 Ki = 8.0 nM 8.10
CHEMBL189910 Ki = 42.0 nM 7.38