Assay Detail

CHEMBL763828

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Functional

Inhibition of HDJ2 farnesylation in PSN-1 cells over 7 hr assay

ChEMBL ↗

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Target

Protein farnesyltransferase (CHEMBL2094108) ↗

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Protein farnesyltransferase (CHEMBL2094108) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Protein farnesyltransferase

CHEMBL2094108

Anchored from Assay target.

Protein identity Protein farnesyltransferase

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

Protein farnesyltransferase (CHEMBL2094108) ↗

Type	PROTEIN COMPLEX
Organism	Homo sapiens

Publication

3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.

Bell IM, Gallicchio SN, Abrams M, Beese LS, Beshore DC, Bhimnathwala H, Bogusky MJ, Buser CA, Culberson JC, Davide J, Ellis-Hutchings M, Fernandes C, Gibbs JB, Graham SL, Hamilton KA, Hartman GD, Heimbrook DC, Homnick CF, Huber HE, Huff JR, Kassahun K, Koblan KS, Kohl NE, Lobell RB, Lynch JJ, Robinson R, Rodrigues AD, Taylor JS, Walsh ES, Williams TM, Zartman CB.
J Med Chem (2002) 45 : 2388 -2409
PubMed 12036349 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	1	8.26	8.26

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL80702	—	—	1	8.26

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL80702	—	EC50	=	5.5	nM	8.26