Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name
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ligand
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selectivity
# Tested
GPCRs
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p-value
(-log)
Activity
Type
Activity
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Activity
Value
AssayType

Assay
Description
Source

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weight
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DOI

6433 10629 0 None -10 2 Human 5.9 pIC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 563 10 4 9 2.2 COc1ccc(cc1)Cn1c(NCCNC(=N)NC(=O)c2ccc(cc2)F)nc(=O)n(c1=O)Cc1ccc(cc1)F 21421710
73755221 10629 0 None -10 2 Human 5.9 pIC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 563 10 4 9 2.2 COc1ccc(cc1)Cn1c(NCCNC(=N)NC(=O)c2ccc(cc2)F)nc(=O)n(c1=O)Cc1ccc(cc1)F 21421710
1866 9952 0 None 1 2 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12054613
1866 9952 0 None 1 2 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15772293
16122905 9909 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 438 7 0 5 3.7 CC(CN(C(=O)C1OCCN(C1)Cc1ccccc1)Cc1ccc2c(c1)OCCCO2)C 22431614
6066 9909 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 438 7 0 5 3.7 CC(CN(C(=O)C1OCCN(C1)Cc1ccccc1)Cc1ccc2c(c1)OCCCO2)C 22431614
1867 9953 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12054613
1867 9953 0 None -1 2 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15772293
1865 9321 0 None 6 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12054613
1868 9955 0 None -31 2 Human 6.0 pIC50 > 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15772293




Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Similar-
ity
Common
name
GPCRdb
ID
#Vendors

Reference
ligand
Fold
selectivity
# Tested
GPCRs
Species

p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Assay
Type
Assay
Description
Source

Mol
weight
Rot
Bonds
H don

H acc

LogP

Smiles

DOI

11951384 10628 0 None -74 2 Human 5.8 pKi = 5.8 Binding
Displacement of [I125]MIT from PKR2 expressed in CHO cell membraneDisplacement of [I125]MIT from PKR2 expressed in CHO cell membrane
ChEMBL 451 10 3 8 0.8 CCc1ccc(cc1)Cn1c(=O)nc(n(c1=O)Cc1ccc(cc1)OC)NCCN=C(N)N 10.1021/jm800854e
6064 10628 0 None -74 2 Human 5.8 pKi = 5.8 Binding
Displacement of [I125]MIT from PKR2 expressed in CHO cell membraneDisplacement of [I125]MIT from PKR2 expressed in CHO cell membrane
ChEMBL 451 10 3 8 0.8 CCc1ccc(cc1)Cn1c(=O)nc(n(c1=O)Cc1ccc(cc1)OC)NCCN=C(N)N 10.1021/jm800854e
CHEMBL457515 10628 0 None -74 2 Human 5.8 pKi = 5.8 Binding
Displacement of [I125]MIT from PKR2 expressed in CHO cell membraneDisplacement of [I125]MIT from PKR2 expressed in CHO cell membrane
ChEMBL 451 10 3 8 0.8 CCc1ccc(cc1)Cn1c(=O)nc(n(c1=O)Cc1ccc(cc1)OC)NCCN=C(N)N 10.1021/jm800854e
25138121 196402 0 None -53 2 Human 4.6 pKi = 4.6 Binding
Displacement of [I125]MIT from PKR2 expressed in CHO cell membraneDisplacement of [I125]MIT from PKR2 expressed in CHO cell membrane
ChEMBL 409 9 2 8 1.4 CCc1ccc(Cn2c(=O)nc(NCCN)n(Cc3ccc(OC)cc3)c2=O)cc1 10.1021/jm800854e
CHEMBL514895 196402 0 None -53 2 Human 4.6 pKi = 4.6 Binding
Displacement of [I125]MIT from PKR2 expressed in CHO cell membraneDisplacement of [I125]MIT from PKR2 expressed in CHO cell membrane
ChEMBL 409 9 2 8 1.4 CCc1ccc(Cn2c(=O)nc(NCCN)n(Cc3ccc(OC)cc3)c2=O)cc1 10.1021/jm800854e
25138122 182878 0 None -15 2 Human 4.2 pKi = 4.2 Binding
Displacement of [I125]MIT from PKR2 expressed in CHO cell membraneDisplacement of [I125]MIT from PKR2 expressed in CHO cell membrane
ChEMBL 477 10 3 10 1.0 CCc1ccc(Cn2c(=O)nc(NCCNC3=NCCN3)n(Cc3ccc(OC)cc3)c2=O)cc1 10.1021/jm800854e
CHEMBL459142 182878 0 None -15 2 Human 4.2 pKi = 4.2 Binding
Displacement of [I125]MIT from PKR2 expressed in CHO cell membraneDisplacement of [I125]MIT from PKR2 expressed in CHO cell membrane
ChEMBL 477 10 3 10 1.0 CCc1ccc(Cn2c(=O)nc(NCCNC3=NCCN3)n(Cc3ccc(OC)cc3)c2=O)cc1 10.1021/jm800854e
11951384 10628 0 None -74 2 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 10 3 8 0.8 CCc1ccc(cc1)Cn1c(=O)nc(n(c1=O)Cc1ccc(cc1)OC)NCCN=C(N)N 19006379
6064 10628 0 None -74 2 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 10 3 8 0.8 CCc1ccc(cc1)Cn1c(=O)nc(n(c1=O)Cc1ccc(cc1)OC)NCCN=C(N)N 19006379
CHEMBL457515 10628 0 None -74 2 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 10 3 8 0.8 CCc1ccc(cc1)Cn1c(=O)nc(n(c1=O)Cc1ccc(cc1)OC)NCCN=C(N)N 19006379