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Assay Detail

CHEMBL681803

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Binding
In vitro inhibitory activity was evaluated against farnesyltransferase (FTase)
27
Total Activities
27
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

Potent and orally bioavailable noncysteine-containing inhibitors of protein farnesyltransferase.
Augeri DJ, Janowick D, Kalvin D, Sullivan G, Larsen J, Dickman D, Ding H, Cohen J, Lee J, Warner R, Kovar P, Cherian S, Saeed B, Zhang H, Tahir S, Ng SC, Sham H, Rosenberg SH.
Bioorg Med Chem Lett (1999) 9 : 1069 -1074
PubMed 10328287 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 8.32 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274122 1 9.40
CHEMBL54044 1 9.30
CHEMBL10877 1 9.15
CHEMBL417606 1 8.92
CHEMBL273697 1 8.82
CHEMBL10912 1 8.62
CHEMBL11210 1 8.59
CHEMBL276602 1 8.54
CHEMBL10990 1 8.54
CHEMBL428001 1 8.52
CHEMBL430296 1 8.52
CHEMBL10812 1 8.31
CHEMBL10955 1 8.22
CHEMBL430096 1 8.22
CHEMBL11003 1 8.21
CHEMBL10970 1 8.20
CHEMBL10902 1 8.19
CHEMBL430307 1 8.18
CHEMBL11195 1 8.12
CHEMBL273265 1 8.08
CHEMBL273507 1 8.06
CHEMBL274672 1 8.00
CHEMBL273721 1 7.92
CHEMBL10762 1 7.72
CHEMBL10687 1 7.70
CHEMBL10572 1 6.25
CHEMBL266618 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274122 IC50 = 0.4 nM 9.40
CHEMBL54044 IC50 = 0.5 nM 9.30
CHEMBL10877 IC50 = 0.7 nM 9.15
CHEMBL417606 IC50 = 1.2 nM 8.92
CHEMBL273697 IC50 = 1.5 nM 8.82
CHEMBL10912 IC50 = 2.4 nM 8.62
CHEMBL11210 IC50 = 2.6 nM 8.59
CHEMBL276602 IC50 = 2.9 nM 8.54
CHEMBL10990 IC50 = 2.9 nM 8.54
CHEMBL428001 IC50 = 3.0 nM 8.52
CHEMBL430296 IC50 = 3.0 nM 8.52
CHEMBL10812 IC50 = 4.9 nM 8.31
CHEMBL10955 IC50 = 6.0 nM 8.22
CHEMBL430096 IC50 = 6.0 nM 8.22
CHEMBL11003 IC50 = 6.2 nM 8.21
CHEMBL10970 IC50 = 6.3 nM 8.20
CHEMBL10902 IC50 = 6.5 nM 8.19
CHEMBL430307 IC50 = 6.6 nM 8.18
CHEMBL11195 IC50 = 7.6 nM 8.12
CHEMBL273265 IC50 = 8.4 nM 8.08
CHEMBL273507 IC50 = 8.8 nM 8.06
CHEMBL274672 IC50 = 9.9 nM 8.00
CHEMBL273721 IC50 = 12.0 nM 7.92
CHEMBL10762 IC50 = 19.0 nM 7.72
CHEMBL10687 IC50 = 20.0 nM 7.70
CHEMBL10572 IC50 = 560.0 nM 6.25
CHEMBL266618 IC50 > 1000.0 nM -