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Assay Detail

CHEMBL828044

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Binding
Inhibition of Bovine farnesyl transferase
ChEMBL ↗
68
Total Activities
67
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2095178) ↗
Type PROTEIN COMPLEX
Organism Bos taurus

Publication

Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase.
Wang GT, Wang X, Wang W, Hasvold LA, Sullivan G, Hutchins CW, O'Conner S, Gentiles R, Sowin T, Cohen J, Gu WZ, Zhang H, Rosenberg SH, Sham HL.
Bioorg Med Chem Lett (2005) 15 : 153 -158
PubMed 15582430 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 68 7.99 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41748 — — 1 9.70
CHEMBL360525 — — 1 9.10
CHEMBL29982 — — 1 8.96
CHEMBL359959 — — 1 8.92
CHEMBL183719 — — 1 8.89
CHEMBL179902 — — 1 8.89
CHEMBL183832 — — 1 8.89
CHEMBL183276 — — 1 8.82
CHEMBL183097 — — 1 8.77
CHEMBL361353 — — 1 8.77
CHEMBL183356 — — 1 8.74
CHEMBL182330 — — 1 8.72
CHEMBL368904 — — 1 8.70
CHEMBL182679 — — 1 8.68
CHEMBL183224 — — 1 8.59
CHEMBL181318 — — 1 8.57
CHEMBL183902 — — 1 8.46
CHEMBL183523 — — 1 8.44
CHEMBL182978 — — 2 8.40
CHEMBL361357 — — 1 8.39
CHEMBL183725 — — 1 8.26
CHEMBL182812 — — 1 8.21
CHEMBL182925 — — 1 8.21
CHEMBL183372 — — 1 8.12
CHEMBL183666 — — 1 8.12
CHEMBL360694 — — 1 8.11
CHEMBL183290 — — 1 8.09
CHEMBL180550 — — 1 8.08
CHEMBL179857 — — 1 8.05
CHEMBL359950 — — 1 8.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41748 — IC50 = 0.2 nM 9.70
CHEMBL360525 — IC50 = 0.8 nM 9.10
CHEMBL29982 — IC50 = 1.1 nM 8.96
CHEMBL359959 — IC50 = 1.2 nM 8.92
CHEMBL183719 — IC50 = 1.3 nM 8.89
CHEMBL179902 — IC50 = 1.3 nM 8.89
CHEMBL183832 — IC50 = 1.3 nM 8.89
CHEMBL183276 — IC50 = 1.5 nM 8.82
CHEMBL183097 — IC50 = 1.7 nM 8.77
CHEMBL361353 — IC50 = 1.7 nM 8.77
CHEMBL183356 — IC50 = 1.8 nM 8.74
CHEMBL182330 — IC50 = 1.9 nM 8.72
CHEMBL368904 — IC50 = 2.0 nM 8.70
CHEMBL182679 — IC50 = 2.1 nM 8.68
CHEMBL183224 — IC50 = 2.6 nM 8.59
CHEMBL181318 — IC50 = 2.7 nM 8.57
CHEMBL183902 — IC50 = 3.5 nM 8.46
CHEMBL183523 — IC50 = 3.6 nM 8.44
CHEMBL182978 — IC50 = 4.0 nM 8.40
CHEMBL361357 — IC50 = 4.1 nM 8.39
CHEMBL182978 — IC50 = 4.8 nM 8.32
CHEMBL183725 — IC50 = 5.5 nM 8.26
CHEMBL182812 — IC50 = 6.1 nM 8.21
CHEMBL182925 — IC50 = 6.1 nM 8.21
CHEMBL183666 — IC50 = 7.5 nM 8.12
CHEMBL183372 — IC50 = 7.5 nM 8.12
CHEMBL360694 — IC50 = 7.7 nM 8.11
CHEMBL183290 — IC50 = 8.1 nM 8.09
CHEMBL180550 — IC50 = 8.3 nM 8.08
CHEMBL179857 — IC50 = 9.0 nM 8.05
CHEMBL359950 — IC50 = 9.1 nM 8.04
CHEMBL182180 — IC50 = 10.0 nM 8.00
CHEMBL262819 — IC50 = 11.0 nM 7.96
CHEMBL183140 — IC50 = 12.0 nM 7.92
CHEMBL180754 — IC50 = 12.0 nM 7.92
CHEMBL183480 — IC50 = 13.0 nM 7.89
CHEMBL362381 — IC50 = 13.0 nM 7.89
CHEMBL361616 — IC50 = 13.0 nM 7.89
CHEMBL183291 — IC50 = 13.0 nM 7.89
CHEMBL183548 — IC50 = 14.0 nM 7.85
CHEMBL360574 — IC50 = 15.0 nM 7.82
CHEMBL180139 — IC50 = 16.0 nM 7.80
CHEMBL182389 — IC50 = 17.0 nM 7.77
CHEMBL181901 — IC50 = 18.0 nM 7.75
CHEMBL362174 — IC50 = 19.0 nM 7.72
CHEMBL182512 — IC50 = 19.0 nM 7.72
CHEMBL180536 — IC50 = 20.0 nM 7.70
CHEMBL369304 — IC50 = 27.0 nM 7.57
CHEMBL426961 — IC50 = 29.0 nM 7.54
CHEMBL362044 — IC50 = 32.0 nM 7.50