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Assay Detail

CHEMBL936745

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

Binding
Inhibition of recombinant wild-type glucocerebrosidase
ChEMBL ↗
52
Total Activities
27
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Lysosomal acid glucosylceramidase (CHEMBL2179) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Three classes of glucocerebrosidase inhibitors identified by quantitative high-throughput screening are chaperone leads for Gaucher disease.
Zheng W, Padia J, Urban DJ, Jadhav A, Goker-Alpan O, Simeonov A, Goldin E, Auld D, LaMarca ME, Inglese J, Austin CP, Sidransky E.
Proc Natl Acad Sci U S A (2007) 104 : 13192 -13197
PubMed 17670938 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 5.83 7.51
Ki 25 6.09 7.68
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL403714 — — 2 7.68
CHEMBL406121 — — 2 7.28
CHEMBL259854 — — 2 7.26
CHEMBL259853 — — 2 7.25
CHEMBL408500 — — 1 6.99
CHEMBL260582 — — 2 6.99
CHEMBL406704 — — 2 6.92
CHEMBL260291 — — 2 6.92
CHEMBL260290 — — 2 6.74
CHEMBL429079 — — 2 6.50
CHEMBL258515 — — 2 6.29
CHEMBL264147 — — 2 6.25
CHEMBL259330 — — 2 6.01
CHEMBL236065 — — 2 5.56
CHEMBL262347 — — 2 5.53
CHEMBL236275 — — 2 5.37
CHEMBL264146 — — 2 5.19
CHEMBL402477 — — 2 5.15
CHEMBL261397 — — 1 4.78
CHEMBL405616 — — 2 4.72
CHEMBL264148 — — 2 4.63
CHEMBL406884 — — 2 4.33
CHEMBL259717 — — 2 4.32
CHEMBL259848 — — 2 4.30
CHEMBL448107 — — 2 -
CHEMBL259147 — — 2 -
CHEMBL261133 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL403714 — Ki = 21.0 nM 7.68
CHEMBL403714 — IC50 = 31.0 nM 7.51
CHEMBL406121 — Ki = 52.0 nM 7.28
CHEMBL259854 — Ki = 55.0 nM 7.26
CHEMBL259853 — Ki = 56.0 nM 7.25
CHEMBL259853 — IC50 = 63.0 nM 7.20
CHEMBL408500 — IC50 = 103.0 nM 6.99
CHEMBL406121 — IC50 = 103.0 nM 6.99
CHEMBL260582 — Ki = 102.0 nM 6.99
CHEMBL260291 — Ki = 121.0 nM 6.92
CHEMBL406704 — Ki = 120.0 nM 6.92
CHEMBL259854 — IC50 = 133.0 nM 6.88
CHEMBL260582 — IC50 = 168.0 nM 6.78
CHEMBL260290 — Ki = 184.0 nM 6.74
CHEMBL260291 — IC50 = 183.0 nM 6.74
CHEMBL406704 — IC50 = 268.0 nM 6.57
CHEMBL429079 — Ki = 320.0 nM 6.50
CHEMBL429079 — IC50 = 430.0 nM 6.37
CHEMBL260290 — IC50 = 452.0 nM 6.34
CHEMBL258515 — Ki = 514.0 nM 6.29
CHEMBL264147 — Ki = 556.0 nM 6.25
CHEMBL259330 — Ki = 975.0 nM 6.01
CHEMBL258515 — IC50 = 1060.0 nM 5.97
CHEMBL264147 — IC50 = 1290.0 nM 5.89
CHEMBL259330 — IC50 = 2450.0 nM 5.61
CHEMBL236065 — Ki = 2780.0 nM 5.56
CHEMBL262347 — IC50 = 2960.0 nM 5.53
CHEMBL236065 — IC50 = 4310.0 nM 5.37
CHEMBL236275 — Ki = 4230.0 nM 5.37
CHEMBL264146 — IC50 = 6460.0 nM 5.19
CHEMBL402477 — Ki = 7150.0 nM 5.15
CHEMBL236275 — IC50 = 7730.0 nM 5.11
CHEMBL262347 — Ki = 8440.0 nM 5.07
CHEMBL264146 — Ki = 13400.0 nM 4.87
CHEMBL261397 — IC50 = 16700.0 nM 4.78
CHEMBL405616 — Ki = 19200.0 nM 4.72
CHEMBL264148 — Ki = 23400.0 nM 4.63
CHEMBL402477 — IC50 = 24600.0 nM 4.61
CHEMBL405616 — IC50 = 25200.0 nM 4.60
CHEMBL264148 — IC50 = 34400.0 nM 4.46
CHEMBL406884 — IC50 = 46500.0 nM 4.33
CHEMBL259717 — IC50 = 47700.0 nM 4.32
CHEMBL259848 — Ki = 50600.0 nM 4.30
CHEMBL448107 — Ki = 122000.0 nM -
CHEMBL259717 — Ki - — -
CHEMBL406884 — Ki - — -
CHEMBL259147 — IC50 - — -
CHEMBL448107 — Activity - — -
CHEMBL261133 — IC50 - — -
CHEMBL261133 — Ki - — -