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Assay Detail

CHEMBL681296

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

Binding
In vitro inhibition of farnesyltransferase farnesylation of the H-ras oncogene
ChEMBL ↗
157
Total Activities
156
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

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 157 6.01 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL368295 — — 1 7.92
CHEMBL305798 — — 1 7.64
CHEMBL432911 — — 1 7.58
CHEMBL169867 — — 1 7.57
CHEMBL367172 — — 1 7.55
CHEMBL354588 — — 1 7.47
CHEMBL352653 — — 1 7.39
CHEMBL306428 — — 1 7.37
CHEMBL353495 — — 1 7.35
CHEMBL171265 — — 1 7.33
CHEMBL355022 — — 1 7.32
CHEMBL144031 — — 1 7.31
CHEMBL305431 — — 1 7.30
CHEMBL369047 — — 1 7.30
CHEMBL354809 — — 1 7.27
CHEMBL171164 — — 1 7.27
CHEMBL366550 — — 1 7.22
CHEMBL170921 — — 1 7.16
CHEMBL352918 — — 1 7.14
CHEMBL167889 — — 1 7.11
CHEMBL170455 — — 1 7.08
CHEMBL171976 — — 1 7.06
CHEMBL171097 — — 1 7.04
CHEMBL172097 — — 1 7.00
CHEMBL172387 — — 1 7.00
CHEMBL354747 — — 1 6.99
CHEMBL170428 — — 1 6.98
CHEMBL170652 — — 1 6.97
CHEMBL352525 — — 1 6.92
CHEMBL66699 — — 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL368295 — IC50 = 12.0 nM 7.92
CHEMBL305798 — IC50 = 23.0 nM 7.64
CHEMBL432911 — IC50 = 26.0 nM 7.58
CHEMBL169867 — IC50 = 27.0 nM 7.57
CHEMBL367172 — IC50 = 28.0 nM 7.55
CHEMBL354588 — IC50 = 34.0 nM 7.47
CHEMBL352653 — IC50 = 41.0 nM 7.39
CHEMBL306428 — IC50 = 43.0 nM 7.37
CHEMBL353495 — IC50 = 45.0 nM 7.35
CHEMBL171265 — IC50 = 47.0 nM 7.33
CHEMBL355022 — IC50 = 48.0 nM 7.32
CHEMBL144031 — IC50 = 49.0 nM 7.31
CHEMBL369047 — IC50 = 50.0 nM 7.30
CHEMBL305431 — IC50 = 50.0 nM 7.30
CHEMBL171164 — IC50 = 54.0 nM 7.27
CHEMBL354809 — IC50 = 54.0 nM 7.27
CHEMBL366550 — IC50 = 60.0 nM 7.22
CHEMBL170921 — IC50 = 69.0 nM 7.16
CHEMBL352918 — IC50 = 72.0 nM 7.14
CHEMBL167889 — IC50 = 78.0 nM 7.11
CHEMBL170455 — IC50 = 83.0 nM 7.08
CHEMBL171976 — IC50 = 87.0 nM 7.06
CHEMBL171097 — IC50 = 92.0 nM 7.04
CHEMBL172387 — IC50 = 100.0 nM 7.00
CHEMBL172097 — IC50 = 100.0 nM 7.00
CHEMBL354747 — IC50 = 102.0 nM 6.99
CHEMBL170428 — IC50 = 104.0 nM 6.98
CHEMBL170652 — IC50 = 108.0 nM 6.97
CHEMBL352525 — IC50 = 120.0 nM 6.92
CHEMBL66699 — IC50 = 140.0 nM 6.85
CHEMBL311310 — IC50 = 160.0 nM 6.80
CHEMBL355453 — IC50 = 170.0 nM 6.77
CHEMBL352324 — IC50 = 190.0 nM 6.72
CHEMBL425133 — IC50 = 210.0 nM 6.68
CHEMBL170887 — IC50 = 210.0 nM 6.68
CHEMBL355101 — IC50 = 230.0 nM 6.64
CHEMBL169130 — IC50 = 240.0 nM 6.62
CHEMBL352727 — IC50 = 280.0 nM 6.55
CHEMBL355483 — IC50 = 300.0 nM 6.52
CHEMBL353906 — IC50 = 300.0 nM 6.52
CHEMBL169934 — IC50 = 310.0 nM 6.51
CHEMBL369265 — IC50 = 330.0 nM 6.48
CHEMBL354131 — IC50 = 340.0 nM 6.47
CHEMBL341393 — IC50 = 360.0 nM 6.44
CHEMBL171484 — IC50 = 380.0 nM 6.42
CHEMBL171785 — IC50 = 390.0 nM 6.41
CHEMBL171463 — IC50 = 400.0 nM 6.40
CHEMBL170014 — IC50 = 450.0 nM 6.35
CHEMBL352600 — IC50 = 460.0 nM 6.34
CHEMBL171210 — IC50 = 470.0 nM 6.33