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Assay Detail

CHEMBL679530

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

Binding
Compound ability to inhibit the transfer of [3H]- farnesyl from Farnesyltransferase to H-Ras-CVLS, a process that is mediated by FPT
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2094108)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent.
Njoroge FG, Taveras AG, Kelly J, Remiszewski S, Mallams AK, Wolin R, Afonso A, Cooper AB, Rane DF, Liu YT, Wong J, Vibulbhan B, Pinto P, Deskus J, Alvarez CS, del Rosario J, Connolly M, Wang J, Desai J, Rossman RR, Bishop WR, Patton R, Wang L, Kirschmeier P, Ganguly AK.
J Med Chem (1998) 41 : 4890 -4902
PubMed 9822558 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.93 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333864 1 8.89
CHEMBL357148 1 8.74
CHEMBL298734 LONAFARNIB 4.0 1 8.72
CHEMBL344068 1 8.64
CHEMBL358796 1 8.60
CHEMBL356519 1 8.59
CHEMBL342099 1 8.51
CHEMBL69954 1 8.30
CHEMBL343845 1 8.22
CHEMBL144337 1 7.78
CHEMBL142724 1 7.48
CHEMBL144031 1 7.31
CHEMBL358047 1 7.21
CHEMBL144029 1 7.11
CHEMBL356935 1 7.07
CHEMBL41934 1 7.05
CHEMBL289404 1 6.60
CHEMBL67405 1 -
CHEMBL343197 1 -
CHEMBL144597 1 -
CHEMBL342349 1 -
CHEMBL358957 1 -
CHEMBL358120 1 -
CHEMBL144202 1 -
CHEMBL356500 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333864 IC50 = 1.3 nM 8.89
CHEMBL357148 IC50 = 1.8 nM 8.74
CHEMBL298734 LONAFARNIB IC50 = 1.9 nM 8.72
CHEMBL344068 IC50 = 2.3 nM 8.64
CHEMBL358796 IC50 = 2.5 nM 8.60
CHEMBL356519 IC50 = 2.6 nM 8.59
CHEMBL342099 IC50 = 3.1 nM 8.51
CHEMBL69954 IC50 = 5.0 nM 8.30
CHEMBL343845 IC50 = 6.0 nM 8.22
CHEMBL144337 IC50 = 16.7 nM 7.78
CHEMBL142724 IC50 = 33.1 nM 7.48
CHEMBL144031 IC50 = 49.0 nM 7.31
CHEMBL358047 IC50 = 62.0 nM 7.21
CHEMBL144029 IC50 = 78.0 nM 7.11
CHEMBL356935 IC50 = 86.0 nM 7.07
CHEMBL41934 IC50 = 90.0 nM 7.05
CHEMBL289404 IC50 = 250.0 nM 6.60
CHEMBL67405 IC50 > 94.0 nM -
CHEMBL343197 IC50 > 88.0 nM -
CHEMBL144597 IC50 > 280.0 nM -
CHEMBL342349 IC50 > 95.0 nM -
CHEMBL358957 IC50 < 3.8 nM -
CHEMBL358120 IC50 > 99.0 nM -
CHEMBL144202 IC50 > 94.0 nM -
CHEMBL356500 IC50 > 110.0 nM -