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Assay Detail

CHEMBL750321

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

Functional
Compound ability to inhibit anchorage-independent growth of NIH-H tumor cell lines in soft agar.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NIH-H
Confidence 1 — Organism
Curated By Intermediate

Target

NIH-H (CHEMBL615000)
Type CELL-LINE

Publication

(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent.
Njoroge FG, Taveras AG, Kelly J, Remiszewski S, Mallams AK, Wolin R, Afonso A, Cooper AB, Rane DF, Liu YT, Wong J, Vibulbhan B, Pinto P, Deskus J, Alvarez CS, del Rosario J, Connolly M, Wang J, Desai J, Rossman RR, Bishop WR, Patton R, Wang L, Kirschmeier P, Ganguly AK.
J Med Chem (1998) 41 : 4890 -4902
PubMed 9822558 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.67 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333864 1 7.30
CHEMBL298734 LONAFARNIB 4.0 1 7.14
CHEMBL358957 1 6.70
CHEMBL342099 1 6.60
CHEMBL358796 1 6.54
CHEMBL69954 1 6.30
CHEMBL344068 1 6.12
CHEMBL357148 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333864 IC50 = 50.0 nM 7.30
CHEMBL298734 LONAFARNIB IC50 = 72.0 nM 7.14
CHEMBL358957 IC50 = 200.0 nM 6.70
CHEMBL342099 IC50 = 250.0 nM 6.60
CHEMBL358796 IC50 = 286.0 nM 6.54
CHEMBL69954 IC50 = 500.0 nM 6.30
CHEMBL344068 IC50 = 750.0 nM 6.12
CHEMBL357148 IC50 < 50.0 nM -