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Assay Detail

CHEMBL677851

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Binding
Concentration required for the inhibitory activity against human Farnesyltransferase
ChEMBL ↗
45
Total Activities
45
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

2-Arylindole-3-acetamides: FPP-competitive inhibitors of farnesyl protein transferase.
Trotter BW, Quigley AG, Lumma WC, Sisko JT, Walsh ES, Hamann CS, Robinson RG, Bhimnathwala H, Kolodin DG, Zheng W, Buser CA, Huber HE, Lobell RB, Kohl NE, Williams TM, Graham SL, Dinsmore CJ.
Bioorg Med Chem Lett (2001) 11 : 865 -869
PubMed 11294379 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 6.30 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL354677 — — 1 7.92
CHEMBL355551 — — 1 7.82
CHEMBL169607 — — 1 7.51
CHEMBL355028 — — 1 7.39
CHEMBL353493 — — 1 7.36
CHEMBL169986 — — 1 7.35
CHEMBL165823 — — 1 7.34
CHEMBL352665 — — 1 7.24
CHEMBL1788269 — — 1 7.11
CHEMBL355301 — — 1 6.97
CHEMBL355842 — — 1 6.96
CHEMBL169069 — — 1 6.91
CHEMBL169326 — — 1 6.80
CHEMBL171214 — — 1 6.77
CHEMBL169197 — — 1 6.76
CHEMBL353398 — — 1 6.74
CHEMBL433529 — — 1 6.63
CHEMBL169997 — — 1 6.62
CHEMBL355654 — — 1 6.61
CHEMBL169374 — — 1 6.42
CHEMBL353289 — — 1 6.40
CHEMBL424564 — — 1 6.29
CHEMBL422557 — — 1 6.28
CHEMBL366672 — — 1 6.25
CHEMBL168643 — — 1 6.24
CHEMBL355773 — — 1 6.17
CHEMBL352766 — — 1 6.15
CHEMBL169817 — — 1 5.86
CHEMBL353724 — — 1 5.82
CHEMBL439652 — — 1 5.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL354677 — IC50 = 12.0 nM 7.92
CHEMBL355551 — IC50 = 15.0 nM 7.82
CHEMBL169607 — IC50 = 31.0 nM 7.51
CHEMBL355028 — IC50 = 41.0 nM 7.39
CHEMBL353493 — IC50 = 44.0 nM 7.36
CHEMBL169986 — IC50 = 45.0 nM 7.35
CHEMBL165823 — IC50 = 46.0 nM 7.34
CHEMBL352665 — IC50 = 58.0 nM 7.24
CHEMBL1788269 — IC50 = 77.0 nM 7.11
CHEMBL355301 — IC50 = 106.0 nM 6.97
CHEMBL355842 — IC50 = 110.0 nM 6.96
CHEMBL169069 — IC50 = 123.0 nM 6.91
CHEMBL169326 — IC50 = 160.0 nM 6.80
CHEMBL171214 — IC50 = 171.0 nM 6.77
CHEMBL169197 — IC50 = 172.0 nM 6.76
CHEMBL353398 — IC50 = 182.0 nM 6.74
CHEMBL433529 — IC50 = 232.0 nM 6.63
CHEMBL169997 — IC50 = 241.0 nM 6.62
CHEMBL355654 — IC50 = 245.0 nM 6.61
CHEMBL169374 — IC50 = 380.0 nM 6.42
CHEMBL353289 — IC50 = 400.0 nM 6.40
CHEMBL424564 — IC50 = 517.0 nM 6.29
CHEMBL422557 — IC50 = 527.0 nM 6.28
CHEMBL366672 — IC50 = 568.0 nM 6.25
CHEMBL168643 — IC50 = 572.0 nM 6.24
CHEMBL355773 — IC50 = 684.0 nM 6.17
CHEMBL352766 — IC50 = 712.0 nM 6.15
CHEMBL169817 — IC50 = 1372.0 nM 5.86
CHEMBL353724 — IC50 = 1500.0 nM 5.82
CHEMBL439652 — IC50 = 1628.0 nM 5.79
CHEMBL169495 — IC50 = 1740.0 nM 5.76
CHEMBL168642 — IC50 = 2150.0 nM 5.67
CHEMBL354580 — IC50 = 2484.0 nM 5.61
CHEMBL353834 — IC50 = 2733.0 nM 5.56
CHEMBL352831 — IC50 = 3803.0 nM 5.42
CHEMBL367709 — IC50 = 3900.0 nM 5.41
CHEMBL170889 — IC50 = 4004.0 nM 5.40
CHEMBL1744068 — IC50 = 4588.0 nM 5.34
CHEMBL172464 — IC50 = 8685.0 nM 5.06
CHEMBL353527 — IC50 = 8641.0 nM 5.06
CHEMBL435070 — IC50 = 11389.0 nM 4.94
CHEMBL171230 — IC50 = 14369.0 nM 4.84
CHEMBL354877 — IC50 = 29863.0 nM 4.53
CHEMBL168469 — IC50 > 50000.0 nM -
CHEMBL352341 — IC50 > 50000.0 nM -