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Assay Detail

CHEMBL2175515

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

Binding
Inhibition of RabGGTase using [3H]GGPP as substrate after 1 hr by scintillation proximity assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Development of selective, potent RabGGTase inhibitors.
Stigter EA, Guo Z, Bon RS, Wu YW, Choidas A, Wolf A, Menninger S, Waldmann H, Blankenfeldt W, Goody RS.
J Med Chem (2012) 55 : 8330 -8340
PubMed 22963166 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.90 8.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2171832 1 8.26
CHEMBL2171687 1 8.22
CHEMBL1738728 1 8.19
CHEMBL2171690 1 7.96
CHEMBL2171691 1 7.89
CHEMBL2171843 1 7.81
CHEMBL2171837 1 7.72
CHEMBL2171834 1 7.65
CHEMBL2171842 1 7.63
CHEMBL2171675 1 7.57
CHEMBL2171682 1 7.43
CHEMBL2171684 1 7.26
CHEMBL2171836 1 7.26
CHEMBL2171840 1 7.20
CHEMBL2171674 1 7.15
CHEMBL2171672 1 6.92
CHEMBL2171688 1 6.91
CHEMBL2171839 1 6.81
CHEMBL2171841 1 6.74
CHEMBL2171835 1 6.73
CHEMBL2171676 1 6.61
CHEMBL2171679 1 6.58
CHEMBL2171680 1 6.24
CHEMBL2171831 1 6.15
CHEMBL2171683 1 5.98
CHEMBL2171689 1 5.83
CHEMBL1738867 1 5.81
CHEMBL2171678 1 5.65
CHEMBL2171677 1 5.37
CHEMBL2171685 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2171832 IC50 = 5.5 nM 8.26
CHEMBL2171687 IC50 = 6.0 nM 8.22
CHEMBL1738728 IC50 = 6.4 nM 8.19
CHEMBL2171690 IC50 = 11.0 nM 7.96
CHEMBL2171691 IC50 = 12.8 nM 7.89
CHEMBL2171843 IC50 = 15.5 nM 7.81
CHEMBL2171837 IC50 = 19.0 nM 7.72
CHEMBL2171834 IC50 = 22.5 nM 7.65
CHEMBL2171842 IC50 = 23.5 nM 7.63
CHEMBL2171675 IC50 = 27.0 nM 7.57
CHEMBL2171682 IC50 = 37.0 nM 7.43
CHEMBL2171684 IC50 = 55.0 nM 7.26
CHEMBL2171836 IC50 = 55.0 nM 7.26
CHEMBL2171840 IC50 = 63.0 nM 7.20
CHEMBL2171674 IC50 = 70.5 nM 7.15
CHEMBL2171672 IC50 = 121.3 nM 6.92
CHEMBL2171688 IC50 = 123.0 nM 6.91
CHEMBL2171839 IC50 = 156.0 nM 6.81
CHEMBL2171841 IC50 = 181.0 nM 6.74
CHEMBL2171835 IC50 = 185.0 nM 6.73
CHEMBL2171676 IC50 = 246.5 nM 6.61
CHEMBL2171679 IC50 = 260.0 nM 6.58
CHEMBL2171680 IC50 = 577.0 nM 6.24
CHEMBL2171831 IC50 = 706.0 nM 6.15
CHEMBL2171683 IC50 = 1056.0 nM 5.98
CHEMBL2171689 IC50 = 1496.0 nM 5.83
CHEMBL1738867 IC50 = 1547.0 nM 5.81
CHEMBL2171678 IC50 = 2240.0 nM 5.65
CHEMBL2171677 IC50 = 4292.0 nM 5.37
CHEMBL2171685 IC50 = 5245.0 nM 5.28
CHEMBL2171673 IC50 = 5719.0 nM 5.24
CHEMBL2171830 IC50 < 14.0 nM -
CHEMBL2171681 IC50 - -
CHEMBL2171833 IC50 < 4.0 nM -
CHEMBL2171686 IC50 - -
CHEMBL2171838 IC50 < 4.0 nM -