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Assay Detail

CHEMBL1786744

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Functional
Antagonist activity at rat mGluR1
ChEMBL ↗
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Metabotropic glutamate receptor 1 (CHEMBL4477) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain.
Sasikumar TK, Qiang L, Burnett DA, Greenlee WJ, Li C, Heimark L, Pramanik B, Grilli M, Bertorelli R, Lozza G, Reggiani A.
Bioorg Med Chem Lett (2009) 19 : 3199 -3203
PubMed 19433355 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 51 7.97 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1783868 — — 1 9.70
CHEMBL1783869 — — 1 9.40
CHEMBL1783874 — — 1 9.22
CHEMBL1783861 — — 1 9.15
CHEMBL1784049 — — 1 9.15
CHEMBL1783858 — — 1 8.96
CHEMBL1783860 — — 1 8.96
CHEMBL1783867 — — 1 8.92
CHEMBL1783870 — — 1 8.82
CHEMBL1783875 — — 1 8.80
CHEMBL1784054 — — 1 8.66
CHEMBL1784065 — — 1 8.64
CHEMBL1783859 — — 1 8.57
CHEMBL1784055 — — 1 8.54
CHEMBL1783866 — — 1 8.49
CHEMBL1783876 — — 1 8.46
CHEMBL1784057 — — 1 8.42
CHEMBL1783865 — — 1 8.39
CHEMBL1784067 — — 1 8.36
CHEMBL1783864 — — 1 8.27
CHEMBL1784056 — — 1 8.12
CHEMBL1783863 — — 1 8.11
CHEMBL428909 — — 1 8.10
CHEMBL1784053 — — 1 8.10
CHEMBL1784068 — — 1 8.08
CHEMBL1783871 — — 1 7.89
CHEMBL1783872 — — 1 7.89
CHEMBL1783862 — — 1 7.85
CHEMBL1783873 — — 1 7.85
CHEMBL1784051 — — 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1783868 — Ki = 0.2 nM 9.70
CHEMBL1783869 — Ki = 0.4 nM 9.40
CHEMBL1783874 — Ki = 0.6 nM 9.22
CHEMBL1783861 — Ki = 0.7 nM 9.15
CHEMBL1784049 — Ki = 0.7 nM 9.15
CHEMBL1783858 — Ki = 1.1 nM 8.96
CHEMBL1783860 — Ki = 1.1 nM 8.96
CHEMBL1783867 — Ki = 1.2 nM 8.92
CHEMBL1783870 — Ki = 1.5 nM 8.82
CHEMBL1783875 — Ki = 1.6 nM 8.80
CHEMBL1784054 — Ki = 2.2 nM 8.66
CHEMBL1784065 — Ki = 2.3 nM 8.64
CHEMBL1783859 — Ki = 2.7 nM 8.57
CHEMBL1784055 — Ki = 2.9 nM 8.54
CHEMBL1783866 — Ki = 3.2 nM 8.49
CHEMBL1783876 — Ki = 3.5 nM 8.46
CHEMBL1784057 — Ki = 3.8 nM 8.42
CHEMBL1783865 — Ki = 4.1 nM 8.39
CHEMBL1784067 — Ki = 4.4 nM 8.36
CHEMBL1783864 — Ki = 5.4 nM 8.27
CHEMBL1784056 — Ki = 7.5 nM 8.12
CHEMBL1783863 — Ki = 7.7 nM 8.11
CHEMBL428909 — Ki = 7.9 nM 8.10
CHEMBL1784053 — Ki = 8.0 nM 8.10
CHEMBL1784068 — Ki = 8.3 nM 8.08
CHEMBL1783871 — Ki = 13.0 nM 7.89
CHEMBL1783872 — Ki = 13.0 nM 7.89
CHEMBL1783862 — Ki = 14.0 nM 7.85
CHEMBL1783873 — Ki = 14.0 nM 7.85
CHEMBL1784051 — Ki = 18.0 nM 7.75
CHEMBL1784069 — Ki = 25.0 nM 7.60
CHEMBL1784059 — Ki = 25.0 nM 7.60
CHEMBL1784052 — Ki = 27.0 nM 7.57
CHEMBL1784050 — Ki = 28.0 nM 7.55
CHEMBL1784070 — Ki = 29.0 nM 7.54
CHEMBL1784073 — Ki = 32.0 nM 7.50
CHEMBL1784061 — Ki = 38.0 nM 7.42
CHEMBL1784072 — Ki = 39.0 nM 7.41
CHEMBL1784063 — Ki = 43.0 nM 7.37
CHEMBL1784064 — Ki = 49.0 nM 7.31
CHEMBL1784062 — Ki = 62.0 nM 7.21
CHEMBL1784077 — Ki = 63.0 nM 7.20
CHEMBL1784075 — Ki = 65.0 nM 7.19
CHEMBL1784066 — Ki = 64.0 nM 7.19
CHEMBL1784058 — Ki = 68.0 nM 7.17
CHEMBL1784078 — Ki = 69.0 nM 7.16
CHEMBL1784071 — Ki = 77.0 nM 7.11
CHEMBL1784076 — Ki = 107.0 nM 6.97
CHEMBL1784048 — Ki = 160.0 nM 6.80
CHEMBL1784060 — Ki = 1000.0 nM 6.00