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Assay Detail

CHEMBL683552

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Binding
Inhibitory concentration of geranylgeranyl-protein transferase type I
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Geranylgeranyl transferase type-1 subunit beta (CHEMBL4135)
Type SINGLE PROTEIN
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 48 4.90 6.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL327278 1 6.06
CHEMBL317747 1 5.82
CHEMBL100661 1 5.57
CHEMBL102107 1 5.55
CHEMBL312137 1 5.47
CHEMBL98553 1 5.44
CHEMBL98711 1 5.34
CHEMBL316726 1 5.19
CHEMBL99205 1 5.19
CHEMBL98314 1 5.13
CHEMBL317520 1 4.96
CHEMBL318438 1 4.96
CHEMBL101561 1 4.96
CHEMBL97973 1 4.96
CHEMBL100798 1 4.92
CHEMBL329067 1 4.92
CHEMBL418982 1 4.85
CHEMBL327500 1 4.82
CHEMBL318943 1 4.82
CHEMBL101978 1 4.80
CHEMBL101467 1 4.72
CHEMBL101564 1 4.72
CHEMBL101708 1 4.70
CHEMBL327506 1 4.62
CHEMBL319737 1 4.55
CHEMBL100640 1 4.51
CHEMBL102031 1 4.44
CHEMBL316502 1 4.40
CHEMBL98974 1 4.39
CHEMBL100230 1 4.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL327278 IC50 = 880.0 nM 6.06
CHEMBL317747 IC50 = 1500.0 nM 5.82
CHEMBL100661 IC50 = 2700.0 nM 5.57
CHEMBL102107 IC50 = 2800.0 nM 5.55
CHEMBL312137 IC50 = 3400.0 nM 5.47
CHEMBL98553 IC50 = 3600.0 nM 5.44
CHEMBL98711 IC50 = 4600.0 nM 5.34
CHEMBL316726 IC50 = 6500.0 nM 5.19
CHEMBL99205 IC50 = 6500.0 nM 5.19
CHEMBL98314 IC50 = 7400.0 nM 5.13
CHEMBL97973 IC50 = 11000.0 nM 4.96
CHEMBL101561 IC50 = 11000.0 nM 4.96
CHEMBL318438 IC50 = 11000.0 nM 4.96
CHEMBL317520 IC50 = 11000.0 nM 4.96
CHEMBL329067 IC50 = 12000.0 nM 4.92
CHEMBL100798 IC50 = 12000.0 nM 4.92
CHEMBL418982 IC50 = 14000.0 nM 4.85
CHEMBL327500 IC50 = 15000.0 nM 4.82
CHEMBL318943 IC50 = 15000.0 nM 4.82
CHEMBL101978 IC50 = 16000.0 nM 4.80
CHEMBL101467 IC50 = 19000.0 nM 4.72
CHEMBL101564 IC50 = 19000.0 nM 4.72
CHEMBL101708 IC50 = 20000.0 nM 4.70
CHEMBL327506 IC50 = 24000.0 nM 4.62
CHEMBL319737 IC50 = 28000.0 nM 4.55
CHEMBL100640 IC50 = 31000.0 nM 4.51
CHEMBL102031 IC50 = 36000.0 nM 4.44
CHEMBL316502 IC50 = 40000.0 nM 4.40
CHEMBL98974 IC50 = 41000.0 nM 4.39
CHEMBL100230 IC50 = 41000.0 nM 4.39
CHEMBL99381 IC50 = 42000.0 nM 4.38
CHEMBL100579 IC50 = 46000.0 nM 4.34
CHEMBL97925 IC50 = 46000.0 nM 4.34
CHEMBL420833 IC50 = 48000.0 nM 4.32
CHEMBL317129 IC50 > 50000.0 nM -
CHEMBL99435 IC50 > 20000.0 nM -
CHEMBL98147 IC50 > 50000.0 nM -
CHEMBL101788 IC50 > 50000.0 nM -
CHEMBL327946 IC50 > 50000.0 nM -
CHEMBL99323 IC50 > 50000.0 nM -
CHEMBL98361 IC50 ~ 5100.0 nM -
CHEMBL101509 IC50 > 50000.0 nM -
CHEMBL100566 IC50 > 20000.0 nM -
CHEMBL101106 IC50 > 50000.0 nM -
CHEMBL99371 IC50 > 20000.0 nM -
CHEMBL322007 IC50 > 50000.0 nM -
CHEMBL430478 IC50 > 50000.0 nM -
CHEMBL99650 IC50 > 50000.0 nM -