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Assay Detail

CHEMBL680824

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Binding
Inhibition of farnesyltransferase
30
Total Activities
30
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

Synthesis of N,N'-disubstituted 3-aminobenzo[c] and [d]azepin-2-ones as potent and specific farnesyl transferase inhibitors.
Le Diguarher T, Ortuno JC, Shanks D, Guilbaud N, Pierré A, Raimbaud E, Fauchère JL, Hickman JA, Tucker GC, Casara PJ.
Bioorg Med Chem Lett (2004) 14 : 767 -771
PubMed 14741286 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 7.81 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2110187 1 9.00
CHEMBL351706 BMS-214662 1.0 1 8.89
CHEMBL165895 1 8.52
CHEMBL163739 1 8.40
CHEMBL351004 1 8.22
CHEMBL349613 1 8.22
CHEMBL350736 1 8.10
CHEMBL165285 1 8.10
CHEMBL166353 1 8.05
CHEMBL423799 1 8.00
CHEMBL348819 1 8.00
CHEMBL164116 1 7.89
CHEMBL351288 1 7.82
CHEMBL350401 1 7.82
CHEMBL350803 1 7.77
CHEMBL164286 1 7.75
CHEMBL2110188 1 7.72
CHEMBL424023 1 7.72
CHEMBL349443 1 7.66
CHEMBL434879 1 7.64
CHEMBL350545 1 7.64
CHEMBL162968 1 7.58
CHEMBL165519 1 7.58
CHEMBL348850 1 7.33
CHEMBL164798 1 7.27
CHEMBL165454 1 7.27
CHEMBL349203 1 7.26
CHEMBL349598 1 7.21
CHEMBL165072 1 7.11
CHEMBL348772 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2110187 IC50 = 1.0 nM 9.00
CHEMBL351706 BMS-214662 IC50 = 1.3 nM 8.89
CHEMBL165895 IC50 = 3.0 nM 8.52
CHEMBL163739 IC50 = 4.0 nM 8.40
CHEMBL351004 IC50 = 6.0 nM 8.22
CHEMBL349613 IC50 = 6.0 nM 8.22
CHEMBL350736 IC50 = 8.0 nM 8.10
CHEMBL165285 IC50 = 8.0 nM 8.10
CHEMBL166353 IC50 = 9.0 nM 8.05
CHEMBL423799 IC50 = 10.0 nM 8.00
CHEMBL348819 IC50 = 10.0 nM 8.00
CHEMBL164116 IC50 = 13.0 nM 7.89
CHEMBL351288 IC50 = 15.0 nM 7.82
CHEMBL350401 IC50 = 15.0 nM 7.82
CHEMBL350803 IC50 = 17.0 nM 7.77
CHEMBL164286 IC50 = 18.0 nM 7.75
CHEMBL2110188 IC50 = 19.0 nM 7.72
CHEMBL424023 IC50 = 19.0 nM 7.72
CHEMBL349443 IC50 = 22.0 nM 7.66
CHEMBL434879 IC50 = 23.0 nM 7.64
CHEMBL350545 IC50 = 23.0 nM 7.64
CHEMBL162968 IC50 = 26.0 nM 7.58
CHEMBL165519 IC50 = 26.0 nM 7.58
CHEMBL348850 IC50 = 47.0 nM 7.33
CHEMBL164798 IC50 = 54.0 nM 7.27
CHEMBL165454 IC50 = 54.0 nM 7.27
CHEMBL349203 IC50 = 55.0 nM 7.26
CHEMBL349598 IC50 = 62.0 nM 7.21
CHEMBL165072 IC50 = 78.0 nM 7.11
CHEMBL348772 IC50 = 142.0 nM 6.85