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Assay Detail

CHEMBL756498

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

Functional
Inhibition of geranylgeranylation of Rap1a in PSN-1 cells
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PSN-1
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Geranylgeranyl transferase type I (CHEMBL2095164)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Nguyen DN, Stump CA, Walsh ES, Fernandes C, Davide JP, Ellis-Hutchings M, Robinson RG, Williams TM, Lobell RB, Huber HE, Buser CA.
Bioorg Med Chem Lett (2002) 12 : 1269 -1273
PubMed 11965368 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 5.79 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL23650 1 6.10
CHEMBL23460 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL23650 EC50 = 800.0 nM 6.10
CHEMBL23460 EC50 = 3400.0 nM 5.47