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Assay Detail

CHEMBL680220

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

Binding
Inhibitory activity against Geranylgeranyl transferase type I
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Geranylgeranyl transferase type I (CHEMBL2095164)
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 18 4.98 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL131542 1 6.16
CHEMBL132572 1 5.85
CHEMBL130594 1 5.54
CHEMBL445906 1 5.48
CHEMBL334772 1 5.30
CHEMBL133676 1 5.01
CHEMBL334947 1 4.89
CHEMBL130284 1 4.85
CHEMBL133625 1 4.82
CHEMBL335758 1 4.79
CHEMBL132564 1 4.78
CHEMBL130433 1 4.74
CHEMBL133288 1 4.73
CHEMBL129853 1 4.47
CHEMBL132608 1 4.44
CHEMBL336160 1 4.42
CHEMBL133908 1 4.33
CHEMBL334496 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL131542 IC50 = 700.0 nM 6.16
CHEMBL132572 IC50 = 1400.0 nM 5.85
CHEMBL130594 IC50 = 2900.0 nM 5.54
CHEMBL445906 IC50 = 3300.0 nM 5.48
CHEMBL334772 IC50 = 5000.0 nM 5.30
CHEMBL133676 IC50 = 9800.0 nM 5.01
CHEMBL334947 IC50 = 12900.0 nM 4.89
CHEMBL130284 IC50 = 14200.0 nM 4.85
CHEMBL133625 IC50 = 15000.0 nM 4.82
CHEMBL335758 IC50 = 16200.0 nM 4.79
CHEMBL132564 IC50 = 16800.0 nM 4.78
CHEMBL130433 IC50 = 18300.0 nM 4.74
CHEMBL133288 IC50 = 18800.0 nM 4.73
CHEMBL129853 IC50 = 34100.0 nM 4.47
CHEMBL132608 IC50 = 36500.0 nM 4.44
CHEMBL336160 IC50 = 38000.0 nM 4.42
CHEMBL133908 IC50 = 46800.0 nM 4.33
CHEMBL334496 IC50 > 39000.0 nM -