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Assay Detail

CHEMBL664124

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Functional
inhibition of tumor colony formation in soft agar
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cercopithecidae
Cell Type COS-1
Confidence 1 — Organism
Curated By Expert

Target

COS-1 (CHEMBL614563)
Type CELL-LINE
Organism Chlorocebus aethiops

Publication

Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities.
Taveras AG, Deskus J, Chao J, Vaccaro CJ, Njoroge FG, Vibulbhan B, Pinto P, Remiszewski S, del Rosario J, Doll RJ, Alvarez C, Lalwani T, Mallams AK, Rossman RR, Afonso A, Girijavallabhan VM, Ganguly AK, Pramanik B, Heimark L, Bishop WR, Wang L, Kirschmeier P, James L, Carr D, Liu M.
J Med Chem (1999) 42 : 2651 -2661
PubMed 10411485 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.84 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL423680 1 7.30
CHEMBL92499 1 7.16
CHEMBL88432 1 7.12
CHEMBL298734 LONAFARNIB 4.0 1 7.12
CHEMBL89304 1 7.07
CHEMBL328713 1 7.00
CHEMBL88713 1 7.00
CHEMBL313635 1 7.00
CHEMBL443022 1 6.96
CHEMBL90050 1 6.92
CHEMBL90234 1 6.70
CHEMBL264305 1 6.70
CHEMBL90962 1 6.52
CHEMBL432573 1 6.51
CHEMBL327204 1 6.48
CHEMBL91213 1 6.34
CHEMBL315915 1 6.30
CHEMBL90435 1 -
CHEMBL315402 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL423680 IC50 = 50.0 nM 7.30
CHEMBL92499 IC50 = 70.0 nM 7.16
CHEMBL88432 IC50 = 75.0 nM 7.12
CHEMBL298734 LONAFARNIB IC50 = 75.0 nM 7.12
CHEMBL89304 IC50 = 85.0 nM 7.07
CHEMBL328713 IC50 = 100.0 nM 7.00
CHEMBL88713 IC50 = 100.0 nM 7.00
CHEMBL313635 IC50 = 100.0 nM 7.00
CHEMBL443022 IC50 = 110.0 nM 6.96
CHEMBL90050 IC50 = 120.0 nM 6.92
CHEMBL90234 IC50 = 200.0 nM 6.70
CHEMBL264305 IC50 = 200.0 nM 6.70
CHEMBL90962 IC50 = 300.0 nM 6.52
CHEMBL432573 IC50 = 310.0 nM 6.51
CHEMBL327204 IC50 = 330.0 nM 6.48
CHEMBL91213 IC50 = 460.0 nM 6.34
CHEMBL315915 IC50 = 500.0 nM 6.30
CHEMBL90435 IC50 > 500.0 nM -
CHEMBL315402 IC50 > 500.0 nM -