Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name
GPCRdb
ID
Reference
ligand
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Species

Assay
Type

Activity
Type
Activity
Relation
Activity
Value
p-value
(-log)
Fold
selectivity
Tested
GPCRs
Assay
Description
Source

Mol
weight
Rot
Bonds
H don

H acc

LogP

Smiles

DOI

6433 3857 None 0 Human Functional pIC50 = 5.9 5.9 -10 2
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 3857 None 0 Human Functional pIC50 = 5.9 5.9 -10 2
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 3177 None 0 Human Functional pIC50 = 7.2 7.2 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12054613
1866 3177 None 0 Human Functional pIC50 = 7.2 7.2 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15772293
16122905 3135 None 0 Human Functional pIC50 = 7.3 7.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 438 7 0 5 3.7 CC(CN(C(=O)C1OCCN(C1)Cc1ccccc1)Cc1ccc2c(c1)OCCCO2)C 22431614
6066 3135 None 0 Human Functional pIC50 = 7.3 7.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 438 7 0 5 3.7 CC(CN(C(=O)C1OCCN(C1)Cc1ccccc1)Cc1ccc2c(c1)OCCCO2)C 22431614
1867 3180 None 0 Human Functional pIC50 = 8.2 8.2 -1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12054613
1867 3180 None 0 Human Functional pIC50 = 8.2 8.2 -1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15772293
1865 2543 None 0 Human Functional pIC50 = 9.2 9.2 6 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12054613
1868 3181 None 0 Human Functional pIC50 > 6 6.0 -31 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15772293




Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name
GPCRdb
ID
Reference
ligand
Vendors

Species

Assay
Type
Activity
Type
Activity
Relation
Activity
Value
p-value
(-log)
Fold
selectivity
Tested
GPCRs
Assay
Description
Source

Mol
weight
Rot
Bonds
H don

H acc

LogP

Smiles

DOI

11951384 3856 None 0 Human Binding pKi = 5.8 5.8 -74 2
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 3856 None 0 Human Binding pKi = 5.8 5.8 -74 2
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 3856 None 0 Human Binding pKi = 5.8 5.8 -74 2
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 189732 None 0 Human Binding pKi = 4.6 4.6 -53 2
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 189732 None 0 Human Binding pKi = 4.6 4.6 -53 2
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 176203 None 0 Human Binding pKi = 4.2 4.2 -15 2
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 176203 None 0 Human Binding pKi = 4.2 4.2 -15 2
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 3856 None 0 Human Binding pKi = 5.8 5.8 -74 2
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 3856 None 0 Human Binding pKi = 5.8 5.8 -74 2
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 3856 None 0 Human Binding pKi = 5.8 5.8 -74 2
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