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Assay Detail

CHEMBL681407

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

Functional
Inhibition of Farnesyltransferase catalyzed incorporation of [3H]-FPP into recombinant Ras-CVIM.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Protein farnesyltransferase (CHEMBL2095178)
Type PROTEIN COMPLEX
Organism Bos taurus

Publication

Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Nguyen DN, Stump CA, Walsh ES, Fernandes C, Davide JP, Ellis-Hutchings M, Robinson RG, Williams TM, Lobell RB, Huber HE, Buser CA.
Bioorg Med Chem Lett (2002) 12 : 1269 -1273
PubMed 11965368 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.98 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL23460 1 9.77
CHEMBL23155 1 9.60
CHEMBL23411 1 8.92
CHEMBL277413 1 8.80
CHEMBL279433 L-778123 FREE BASE 1.0 1 8.70
CHEMBL23248 1 8.68
CHEMBL23650 1 8.51
CHEMBL23939 1 8.24
CHEMBL283369 1 8.21
CHEMBL280181 1 8.10
CHEMBL23218 1 8.06
CHEMBL283793 1 7.99
CHEMBL23135 1 7.92
CHEMBL23163 1 7.85
CHEMBL23490 1 7.82
CHEMBL23217 1 7.77
CHEMBL23239 1 7.72
CHEMBL283542 1 7.46
CHEMBL23219 1 7.28
CHEMBL22675 1 6.41
CHEMBL283380 1 6.39
CHEMBL282011 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL23460 IC50 = 0.17 nM 9.77
CHEMBL23155 IC50 = 0.25 nM 9.60
CHEMBL23411 IC50 = 1.2 nM 8.92
CHEMBL277413 IC50 = 1.6 nM 8.80
CHEMBL279433 L-778123 FREE BASE IC50 = 2.0 nM 8.70
CHEMBL23248 IC50 = 2.1 nM 8.68
CHEMBL23650 IC50 = 3.1 nM 8.51
CHEMBL23939 IC50 = 5.7 nM 8.24
CHEMBL283369 IC50 = 6.1 nM 8.21
CHEMBL280181 IC50 = 8.0 nM 8.10
CHEMBL23218 IC50 = 8.7 nM 8.06
CHEMBL283793 IC50 = 10.3 nM 7.99
CHEMBL23135 IC50 = 12.0 nM 7.92
CHEMBL23163 IC50 = 14.0 nM 7.85
CHEMBL23490 IC50 = 15.0 nM 7.82
CHEMBL23217 IC50 = 17.0 nM 7.77
CHEMBL23239 IC50 = 19.0 nM 7.72
CHEMBL283542 IC50 = 35.0 nM 7.46
CHEMBL23219 IC50 = 52.0 nM 7.28
CHEMBL22675 IC50 = 392.0 nM 6.41
CHEMBL283380 IC50 = 410.0 nM 6.39
CHEMBL282011 IC50 = 3500.0 nM 5.46