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Assay Detail

CHEMBL682232

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Binding
Inhibitory activity against recombinant human farnesyltransferase
ChEMBL ↗
82
Total Activities
80
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

Identification of novel farnesyl protein transferase inhibitors using three-dimensional database searching methods.
Kaminski JJ, Rane DF, Snow ME, Weber L, Rothofsky ML, Anderson SD, Lin SL.
J Med Chem (1997) 40 : 4103 -4112
PubMed 9406600 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 82 5.60 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL311310 — — 3 7.85
CHEMBL334635 — — 1 7.22
CHEMBL133121 — — 1 6.80
CHEMBL131542 — — 1 6.70
CHEMBL132564 — — 1 6.70
CHEMBL289404 — — 1 6.60
CHEMBL341393 — — 1 6.44
CHEMBL63804 — — 1 6.28
CHEMBL335685 — — 1 6.22
CHEMBL133676 — — 1 6.16
CHEMBL334694 — — 1 6.16
CHEMBL130433 — — 1 6.16
CHEMBL338697 — — 1 6.10
CHEMBL131739 — — 1 6.06
CHEMBL336597 — — 1 6.03
CHEMBL336370 — — 1 6.02
CHEMBL407455 — — 1 6.00
CHEMBL334749 — — 1 6.00
CHEMBL133908 — — 1 5.96
CHEMBL130284 — — 1 5.96
CHEMBL335101 — — 1 5.94
CHEMBL334947 — — 1 5.92
CHEMBL130362 — — 1 5.89
CHEMBL445906 — — 1 5.89
CHEMBL132608 — — 1 5.89
CHEMBL335517 — — 1 5.89
CHEMBL130594 — — 1 5.85
CHEMBL133288 — — 1 5.85
CHEMBL133625 — — 1 5.82
CHEMBL335758 — — 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL311310 — IC50 = 14.0 nM 7.85
CHEMBL334635 — IC50 = 60.0 nM 7.22
CHEMBL133121 — IC50 = 160.0 nM 6.80
CHEMBL132564 — IC50 = 200.0 nM 6.70
CHEMBL131542 — IC50 = 200.0 nM 6.70
CHEMBL289404 — IC50 = 250.0 nM 6.60
CHEMBL341393 — IC50 = 360.0 nM 6.44
CHEMBL311310 — IC50 = 360.0 nM 6.44
CHEMBL63804 — IC50 = 530.0 nM 6.28
CHEMBL335685 — IC50 = 600.0 nM 6.22
CHEMBL311310 — IC50 = 650.0 nM 6.19
CHEMBL133676 — IC50 = 700.0 nM 6.16
CHEMBL130433 — IC50 = 700.0 nM 6.16
CHEMBL334694 — IC50 = 700.0 nM 6.16
CHEMBL338697 — IC50 = 800.0 nM 6.10
CHEMBL131739 — IC50 = 870.0 nM 6.06
CHEMBL336597 — IC50 = 940.0 nM 6.03
CHEMBL336370 — IC50 = 950.0 nM 6.02
CHEMBL407455 — IC50 = 1000.0 nM 6.00
CHEMBL334749 — IC50 = 1000.0 nM 6.00
CHEMBL133908 — IC50 = 1100.0 nM 5.96
CHEMBL130284 — IC50 = 1100.0 nM 5.96
CHEMBL335101 — IC50 = 1140.0 nM 5.94
CHEMBL334947 — IC50 = 1200.0 nM 5.92
CHEMBL132608 — IC50 = 1300.0 nM 5.89
CHEMBL130362 — IC50 = 1300.0 nM 5.89
CHEMBL335517 — IC50 = 1300.0 nM 5.89
CHEMBL445906 — IC50 = 1300.0 nM 5.89
CHEMBL133288 — IC50 = 1400.0 nM 5.85
CHEMBL130594 — IC50 = 1400.0 nM 5.85
CHEMBL133625 — IC50 = 1500.0 nM 5.82
CHEMBL335758 — IC50 = 1600.0 nM 5.80
CHEMBL442406 — IC50 = 1800.0 nM 5.75
CHEMBL129853 — IC50 = 1800.0 nM 5.75
CHEMBL336160 — IC50 = 2000.0 nM 5.70
CHEMBL335307 — IC50 = 2000.0 nM 5.70
CHEMBL334772 — IC50 = 2000.0 nM 5.70
CHEMBL341184 — IC50 = 2100.0 nM 5.68
CHEMBL132522 — IC50 = 2300.0 nM 5.64
CHEMBL133710 — IC50 = 2300.0 nM 5.64
CHEMBL130256 — IC50 = 2300.0 nM 5.64
CHEMBL130074 — IC50 = 2300.0 nM 5.64
CHEMBL335237 — IC50 = 2500.0 nM 5.60
CHEMBL132572 — IC50 = 2500.0 nM 5.60
CHEMBL131845 — IC50 = 2500.0 nM 5.60
CHEMBL339171 — IC50 = 2500.0 nM 5.60
CHEMBL335871 — IC50 = 2700.0 nM 5.57
CHEMBL337858 — IC50 = 2700.0 nM 5.57
CHEMBL131040 — IC50 = 3200.0 nM 5.50
CHEMBL434429 — IC50 = 4400.0 nM 5.36