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Assay Detail

CHEMBL1108345

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

Functional
Agonist activity at human recombinant S1P1 receptor expressed in CHO cells by GTPgammaS binding assay
69
Total Activities
69
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sphingosine 1-phosphate receptor 1 (CHEMBL4333)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
Bolli MH, Abele S, Binkert C, Bravo R, Buchmann S, Bur D, Gatfield J, Hess P, Kohl C, Mangold C, Mathys B, Menyhart K, Müller C, Nayler O, Scherz M, Schmidt G, Sippel V, Steiner B, Strasser D, Treiber A, Weller T.
J Med Chem (2010) 53 : 4198 -4211
PubMed 20446681 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 69 6.81 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1095833 1 8.04
CHEMBL1096146 PONESIMOD 4.0 1 8.01
CHEMBL1094503 1 8.00
CHEMBL1096873 1 7.96
CHEMBL1097184 1 7.92
CHEMBL1096872 1 7.72
CHEMBL1097809 1 7.51
CHEMBL1095152 1 7.47
CHEMBL1097808 1 7.46
CHEMBL1095995 1 7.43
CHEMBL1098143 1 7.33
CHEMBL1094192 1 7.33
CHEMBL1097807 1 7.27
CHEMBL1094831 1 7.26
CHEMBL1094501 1 7.24
CHEMBL1096676 1 7.24
CHEMBL1096786 1 7.21
CHEMBL1097103 1 7.17
CHEMBL1097535 1 7.14
CHEMBL1098142 1 7.11
CHEMBL1097801 1 7.02
CHEMBL1097800 1 7.01
CHEMBL1098449 1 6.99
CHEMBL1097843 1 6.99
CHEMBL1098447 1 6.99
CHEMBL1098144 1 6.97
CHEMBL1095153 1 6.96
CHEMBL1094213 1 6.95
CHEMBL1098811 1 6.91
CHEMBL1097537 1 6.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1095833 EC50 = 9.1 nM 8.04
CHEMBL1096146 PONESIMOD EC50 = 9.7 nM 8.01
CHEMBL1094503 EC50 = 10.0 nM 8.00
CHEMBL1096873 EC50 = 11.0 nM 7.96
CHEMBL1097184 EC50 = 12.0 nM 7.92
CHEMBL1096872 EC50 = 19.0 nM 7.72
CHEMBL1097809 EC50 = 31.0 nM 7.51
CHEMBL1095152 EC50 = 34.0 nM 7.47
CHEMBL1097808 EC50 = 35.0 nM 7.46
CHEMBL1095995 EC50 = 37.0 nM 7.43
CHEMBL1098143 EC50 = 47.0 nM 7.33
CHEMBL1094192 EC50 = 47.0 nM 7.33
CHEMBL1097807 EC50 = 54.0 nM 7.27
CHEMBL1094831 EC50 = 55.0 nM 7.26
CHEMBL1096676 EC50 = 58.0 nM 7.24
CHEMBL1094501 EC50 = 58.0 nM 7.24
CHEMBL1096786 EC50 = 62.0 nM 7.21
CHEMBL1097103 EC50 = 67.0 nM 7.17
CHEMBL1097535 EC50 = 72.0 nM 7.14
CHEMBL1098142 EC50 = 78.0 nM 7.11
CHEMBL1097801 EC50 = 95.0 nM 7.02
CHEMBL1097800 EC50 = 98.0 nM 7.01
CHEMBL1098449 EC50 = 103.0 nM 6.99
CHEMBL1097843 EC50 = 102.0 nM 6.99
CHEMBL1098447 EC50 = 102.0 nM 6.99
CHEMBL1098144 EC50 = 106.0 nM 6.97
CHEMBL1095153 EC50 = 110.0 nM 6.96
CHEMBL1094213 EC50 = 112.0 nM 6.95
CHEMBL1098811 EC50 = 122.0 nM 6.91
CHEMBL1097537 EC50 = 124.0 nM 6.91
CHEMBL1097182 EC50 = 143.0 nM 6.84
CHEMBL1098203 EC50 = 148.0 nM 6.83
CHEMBL1098448 EC50 = 147.0 nM 6.83
CHEMBL1098467 EC50 = 154.0 nM 6.81
CHEMBL1097536 EC50 = 179.0 nM 6.75
CHEMBL1096788 EC50 = 186.0 nM 6.73
CHEMBL1098770 EC50 = 185.0 nM 6.73
CHEMBL1098450 EC50 = 202.0 nM 6.70
CHEMBL1098200 EC50 = 200.0 nM 6.70
CHEMBL1098201 EC50 = 201.0 nM 6.70
CHEMBL1098013 EC50 = 200.0 nM 6.70
CHEMBL1098202 EC50 = 224.0 nM 6.65
CHEMBL1094885 EC50 = 225.0 nM 6.65
CHEMBL1096478 EC50 = 251.0 nM 6.60
CHEMBL1094699 EC50 = 259.0 nM 6.59
CHEMBL1094502 EC50 = 282.0 nM 6.55
CHEMBL1097803 EC50 = 343.0 nM 6.46
CHEMBL1094834 EC50 = 347.0 nM 6.46
CHEMBL1094247 EC50 = 356.0 nM 6.45
CHEMBL1097529 EC50 = 408.0 nM 6.39