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Assay Detail

CHEMBL681470

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Binding
In vitro inhibition of farnesyl transferase using purified recombinant human enzyme
ChEMBL ↗
50
Total Activities
50
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

Design and biological activity of (S)-4-(5-([1-(3-chlorobenzyl)-2-oxopyrrolidin-3-ylamino]methyl)imidazol-1-ylmethyl)benzonitrile, a 3-aminopyrrolidinone farnesyltransferase inhibitor with excellent cell potency.
Bell IM, Gallicchio SN, Abrams M, Beshore DC, Buser CA, Culberson JC, Davide J, Ellis-Hutchings M, Fernandes C, Gibbs JB, Graham SL, Hartman GD, Heimbrook DC, Homnick CF, Huff JR, Kassahun K, Koblan KS, Kohl NE, Lobell RB, Lynch JJ, Miller PA, Omer CA, Rodrigues AD, Walsh ES, Williams TM.
J Med Chem (2001) 44 : 2933 -2949
PubMed 11520202 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 7.29 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL100661 — — 1 8.89
CHEMBL99381 — — 1 8.82
CHEMBL312137 — — 1 8.72
CHEMBL316726 — — 1 8.60
CHEMBL98361 — — 1 8.32
CHEMBL318438 — — 1 8.28
CHEMBL100798 — — 1 8.22
CHEMBL101788 — — 1 8.21
CHEMBL98147 — — 1 8.12
CHEMBL99205 — — 1 8.08
CHEMBL100566 — — 1 8.00
CHEMBL327278 — — 1 7.96
CHEMBL329067 — — 1 7.82
CHEMBL322007 — — 1 7.77
CHEMBL98553 — — 1 7.75
CHEMBL101561 — — 1 7.68
CHEMBL327500 — — 1 7.60
CHEMBL317520 — — 1 7.57
CHEMBL316502 — — 1 7.54
CHEMBL98711 — — 1 7.38
CHEMBL98974 — — 1 7.37
CHEMBL99371 — — 1 7.37
CHEMBL100579 — — 1 7.31
CHEMBL318943 — — 1 7.29
CHEMBL327946 — — 1 7.28
CHEMBL100415 — — 1 7.27
CHEMBL329732 — — 1 7.23
CHEMBL101564 — — 1 7.19
CHEMBL101708 — — 1 7.17
CHEMBL97925 — — 1 7.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL100661 — IC50 = 1.3 nM 8.89
CHEMBL99381 — IC50 = 1.5 nM 8.82
CHEMBL312137 — IC50 = 1.9 nM 8.72
CHEMBL316726 — IC50 = 2.5 nM 8.60
CHEMBL98361 — IC50 = 4.8 nM 8.32
CHEMBL318438 — IC50 = 5.2 nM 8.28
CHEMBL100798 — IC50 = 6.0 nM 8.22
CHEMBL101788 — IC50 = 6.1 nM 8.21
CHEMBL98147 — IC50 = 7.5 nM 8.12
CHEMBL99205 — IC50 = 8.4 nM 8.08
CHEMBL100566 — IC50 = 10.0 nM 8.00
CHEMBL327278 — IC50 = 11.0 nM 7.96
CHEMBL329067 — IC50 = 15.0 nM 7.82
CHEMBL322007 — IC50 = 17.0 nM 7.77
CHEMBL98553 — IC50 = 18.0 nM 7.75
CHEMBL101561 — IC50 = 21.0 nM 7.68
CHEMBL327500 — IC50 = 25.0 nM 7.60
CHEMBL317520 — IC50 = 27.0 nM 7.57
CHEMBL316502 — IC50 = 29.0 nM 7.54
CHEMBL98711 — IC50 = 42.0 nM 7.38
CHEMBL98974 — IC50 = 43.0 nM 7.37
CHEMBL99371 — IC50 = 43.0 nM 7.37
CHEMBL100579 — IC50 = 49.0 nM 7.31
CHEMBL318943 — IC50 = 51.0 nM 7.29
CHEMBL327946 — IC50 = 52.0 nM 7.28
CHEMBL100415 — IC50 = 54.0 nM 7.27
CHEMBL329732 — IC50 = 59.0 nM 7.23
CHEMBL101564 — IC50 = 65.0 nM 7.19
CHEMBL101708 — IC50 = 67.0 nM 7.17
CHEMBL97925 — IC50 = 74.0 nM 7.13
CHEMBL319737 — IC50 = 83.0 nM 7.08
CHEMBL99435 — IC50 = 85.0 nM 7.07
CHEMBL101467 — IC50 = 89.0 nM 7.05
CHEMBL317129 — IC50 = 100.0 nM 7.00
CHEMBL327506 — IC50 = 110.0 nM 6.96
CHEMBL101978 — IC50 = 120.0 nM 6.92
CHEMBL101106 — IC50 = 150.0 nM 6.82
CHEMBL100230 — IC50 = 200.0 nM 6.70
CHEMBL420833 — IC50 = 230.0 nM 6.64
CHEMBL102107 — IC50 = 240.0 nM 6.62
CHEMBL100640 — IC50 = 250.0 nM 6.60
CHEMBL97973 — IC50 = 250.0 nM 6.60
CHEMBL98314 — IC50 = 270.0 nM 6.57
CHEMBL418982 — IC50 = 280.0 nM 6.55
CHEMBL102031 — IC50 = 370.0 nM 6.43
CHEMBL317747 — IC50 = 380.0 nM 6.42
CHEMBL99323 — IC50 = 980.0 nM 6.01
CHEMBL99650 — IC50 = 2000.0 nM 5.70
CHEMBL430478 — IC50 = 2900.0 nM 5.54
CHEMBL101509 — IC50 = 6800.0 nM 5.17