Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL680249

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

Binding
Inhibition of Farnesyltransferase from Ras-CVLS or Ras-CVLL in Cos-7 monkey kidney cells
ChEMBL ↗
65
Total Activities
65
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Chlorocebus aethiops
Cell Type COS-7
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2094108) ↗
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Inhibitors of farnesyl protein transferase. 4-Amido, 4-carbamoyl, and 4-carboxamido derivatives of 1-(8-chloro-6,11-dihydro-5H-benzo[5,6]- cyclohepta[1,2-b]pyridin-11-yl)piperazine and 1-(3-bromo-8-chloro-6,11- dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperazine.
Mallams AK, Rossman RR, Doll RJ, Girijavallabhan VM, Ganguly AK, Petrin J, Wang L, Patton R, Bishop WR, Carr DM, Kirschmeier P, Catino JJ, Bryant MS, Chen KJ, Korfmacher WA, Nardo C, Wang S, Nomeir AA, Lin CC, Li Z, Chen J, Lee S, Dell J, Lipari P, Liu M.
J Med Chem (1998) 41 : 877 -893
PubMed 9526562 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 65 5.70 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL352525 — — 1 7.00
CHEMBL305798 — — 1 6.90
CHEMBL352918 — — 1 6.77
CHEMBL306428 — — 1 6.46
CHEMBL367172 — — 1 6.46
CHEMBL368295 — — 1 6.42
CHEMBL172387 — — 1 6.35
CHEMBL171265 — — 1 6.35
CHEMBL171463 — — 1 6.35
CHEMBL355022 — — 1 6.30
CHEMBL432911 — — 1 6.30
CHEMBL352653 — — 1 6.28
CHEMBL171976 — — 1 6.25
CHEMBL144031 — — 1 6.23
CHEMBL354747 — — 1 6.23
CHEMBL169867 — — 1 6.22
CHEMBL366550 — — 1 6.20
CHEMBL354809 — — 1 6.16
CHEMBL369047 — — 1 6.12
CHEMBL355453 — — 1 6.07
CHEMBL353906 — — 1 6.05
CHEMBL305431 — — 1 6.05
CHEMBL354221 — — 1 6.05
CHEMBL352930 — — 1 6.03
CHEMBL170428 — — 1 5.98
CHEMBL336370 — — 1 5.89
CHEMBL352324 — — 1 5.89
CHEMBL172097 — — 1 5.82
CHEMBL171097 — — 1 5.77
CHEMBL171484 — — 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL352525 — IC50 = 100.0 nM 7.00
CHEMBL305798 — IC50 = 125.0 nM 6.90
CHEMBL352918 — IC50 = 170.0 nM 6.77
CHEMBL306428 — IC50 = 350.0 nM 6.46
CHEMBL367172 — IC50 = 350.0 nM 6.46
CHEMBL368295 — IC50 = 380.0 nM 6.42
CHEMBL172387 — IC50 = 450.0 nM 6.35
CHEMBL171265 — IC50 = 450.0 nM 6.35
CHEMBL171463 — IC50 = 450.0 nM 6.35
CHEMBL355022 — IC50 = 500.0 nM 6.30
CHEMBL432911 — IC50 = 500.0 nM 6.30
CHEMBL352653 — IC50 = 530.0 nM 6.28
CHEMBL171976 — IC50 = 560.0 nM 6.25
CHEMBL354747 — IC50 = 590.0 nM 6.23
CHEMBL144031 — IC50 = 590.0 nM 6.23
CHEMBL169867 — IC50 = 600.0 nM 6.22
CHEMBL366550 — IC50 = 630.0 nM 6.20
CHEMBL354809 — IC50 = 700.0 nM 6.16
CHEMBL369047 — IC50 = 750.0 nM 6.12
CHEMBL355453 — IC50 = 850.0 nM 6.07
CHEMBL353906 — IC50 = 900.0 nM 6.05
CHEMBL305431 — IC50 = 900.0 nM 6.05
CHEMBL354221 — IC50 = 890.0 nM 6.05
CHEMBL352930 — IC50 = 930.0 nM 6.03
CHEMBL170428 — IC50 = 1050.0 nM 5.98
CHEMBL336370 — IC50 = 1300.0 nM 5.89
CHEMBL352324 — IC50 = 1300.0 nM 5.89
CHEMBL172097 — IC50 = 1500.0 nM 5.82
CHEMBL171097 — IC50 = 1700.0 nM 5.77
CHEMBL171484 — IC50 = 2200.0 nM 5.66
CHEMBL355632 — IC50 = 2400.0 nM 5.62
CHEMBL353854 — IC50 = 2700.0 nM 5.57
CHEMBL353897 — IC50 = 3000.0 nM 5.52
CHEMBL169130 — IC50 = 3600.0 nM 5.44
CHEMBL425133 — IC50 = 3700.0 nM 5.43
CHEMBL311310 — IC50 = 3700.0 nM 5.43
CHEMBL354331 — IC50 = 3700.0 nM 5.43
CHEMBL355044 — IC50 = 3900.0 nM 5.41
CHEMBL130362 — IC50 = 4800.0 nM 5.32
CHEMBL422723 — IC50 = 4900.0 nM 5.31
CHEMBL355335 — IC50 = 5000.0 nM 5.30
CHEMBL171785 — IC50 = 5000.0 nM 5.30
CHEMBL341393 — IC50 = 5000.0 nM 5.30
CHEMBL171443 — IC50 = 5100.0 nM 5.29
CHEMBL171938 — IC50 = 5100.0 nM 5.29
CHEMBL170887 — IC50 = 5800.0 nM 5.24
CHEMBL170014 — IC50 = 5700.0 nM 5.24
CHEMBL352727 — IC50 = 6000.0 nM 5.22
CHEMBL334749 — IC50 = 6220.0 nM 5.21
CHEMBL355717 — IC50 = 6200.0 nM 5.21