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Assay Detail

CHEMBL4371948

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

Binding
Inhibition of rat FFAH expressed in Escherichia coli using AAMCA as substrate incubated for 1 min measured for 50 mins by fluorescence assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Fatty-acid amide hydrolase 1 (CHEMBL3229)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery and evaluation of novel FAAH inhibitors in neuropathic pain model.
Bhuniya D, Kharul RK, Hajare A, Shaikh N, Bhosale S, Balwe S, Begum F, De S, Athavankar S, Joshi D, Madgula V, Joshi K, Raje AA, Meru AV, Magdum A, Mookhtiar KA, Barbhaiya R.
Bioorg Med Chem Lett (2019) 29 : 238 -243
PubMed 30503633 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.40 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1651534 REDAFAMDASTAT 2.0 1 8.24
CHEMBL4438972 1 8.21
CHEMBL4435842 1 8.18
CHEMBL4466424 1 8.05
CHEMBL4474161 1 8.04
CHEMBL4557596 1 7.94
CHEMBL1651524 1 7.94
CHEMBL4593464 1 7.89
CHEMBL4577896 1 7.80
CHEMBL4460120 1 7.76
CHEMBL4560227 1 7.56
CHEMBL4468693 1 7.54
CHEMBL4460637 1 7.50
CHEMBL4562421 1 7.28
CHEMBL4538101 1 7.19
CHEMBL4533398 1 7.09
CHEMBL4575497 1 7.00
CHEMBL4466023 1 6.84
CHEMBL4455597 1 6.71
CHEMBL4456294 1 6.58
CHEMBL4578910 1 5.82
CHEMBL4587800 1 5.64
CHEMBL177577 1 -
CHEMBL4537201 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1651534 REDAFAMDASTAT IC50 = 5.7 nM 8.24
CHEMBL4438972 IC50 = 6.2 nM 8.21
CHEMBL4435842 IC50 = 6.6 nM 8.18
CHEMBL4466424 IC50 = 9.0 nM 8.05
CHEMBL4474161 IC50 = 9.2 nM 8.04
CHEMBL4557596 IC50 = 11.6 nM 7.94
CHEMBL1651524 IC50 = 11.5 nM 7.94
CHEMBL4593464 IC50 = 13.0 nM 7.89
CHEMBL4577896 IC50 = 16.0 nM 7.80
CHEMBL4460120 IC50 = 17.2 nM 7.76
CHEMBL4560227 IC50 = 27.8 nM 7.56
CHEMBL4468693 IC50 = 29.0 nM 7.54
CHEMBL4460637 IC50 = 31.3 nM 7.50
CHEMBL4562421 IC50 = 52.0 nM 7.28
CHEMBL4538101 IC50 = 64.6 nM 7.19
CHEMBL4533398 IC50 = 80.7 nM 7.09
CHEMBL4575497 IC50 = 100.0 nM 7.00
CHEMBL4466023 IC50 = 145.0 nM 6.84
CHEMBL4455597 IC50 = 194.0 nM 6.71
CHEMBL4456294 IC50 = 266.0 nM 6.58
CHEMBL4578910 IC50 = 1500.0 nM 5.82
CHEMBL4587800 IC50 = 2300.0 nM 5.64
CHEMBL177577 IC50 - -
CHEMBL4537201 IC50 - -