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Assay Detail

CHEMBL3077240

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Binding
Antagonist activity at AT1 receptor in Rattus norvegicus (rat) liver
ChEMBL ↗
64
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Angiotensin II receptor (AT-1) type-1 (CHEMBL2094250) ↗
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Comprehensive structureactivity relationship analysis of substituted 5-(biphenyl-4-ylmethyl) pyrazoles derivatives as AT1 selective angiotensin II receptor antagonists: 2D and kNNMFA QSAR approach
Sharma MC, Kohli DV
Med Chem Res (2013) 22 : 2124 -2138
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 64 7.57 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL153268 — — 2 8.66
CHEMBL2283577 — — 2 8.52
CHEMBL153385 — — 2 8.43
CHEMBL345979 — — 2 8.36
CHEMBL357951 — — 2 8.34
CHEMBL153013 — — 2 8.17
CHEMBL356877 — — 2 8.14
CHEMBL2283575 — — 2 8.13
CHEMBL152145 — — 2 8.06
CHEMBL154931 — — 2 8.05
CHEMBL443559 — — 2 8.04
CHEMBL153045 — — 2 8.03
CHEMBL422149 — — 2 8.00
CHEMBL153384 — — 2 8.00
CHEMBL2283572 — — 2 7.92
CHEMBL2283573 — — 2 7.89
CHEMBL2283574 — — 2 7.75
CHEMBL153457 — — 2 7.72
CHEMBL151856 — — 2 7.26
CHEMBL433543 — — 2 7.19
CHEMBL358236 — — 2 7.16
CHEMBL2283472 — — 2 7.13
CHEMBL435640 — — 2 7.13
CHEMBL358445 — — 2 7.11
CHEMBL358396 — — 2 7.03
CHEMBL153453 — — 2 6.96
CHEMBL419963 — — 2 6.92
CHEMBL2283576 — — 2 6.89
CHEMBL348705 — — 2 6.54
CHEMBL440358 — — 2 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL153268 — IC50 = 2.2 nM 8.66
CHEMBL153268 — IC50 = 2.71 nM 8.57
CHEMBL2283577 — IC50 = 3.0 nM 8.52
CHEMBL2283577 — IC50 = 3.006 nM 8.52
CHEMBL153385 — IC50 = 3.7 nM 8.43
CHEMBL153385 — IC50 = 3.707 nM 8.43
CHEMBL345979 — IC50 = 4.4 nM 8.36
CHEMBL345979 — IC50 = 4.406 nM 8.36
CHEMBL357951 — IC50 = 4.6 nM 8.34
CHEMBL357951 — IC50 = 4.603 nM 8.34
CHEMBL153013 — IC50 = 6.7 nM 8.17
CHEMBL153013 — IC50 = 6.714 nM 8.17
CHEMBL356877 — IC50 = 7.311 nM 8.14
CHEMBL356877 — IC50 = 7.3 nM 8.14
CHEMBL2283575 — IC50 = 7.413 nM 8.13
CHEMBL2283575 — IC50 = 7.4 nM 8.13
CHEMBL152145 — IC50 = 8.7 nM 8.06
CHEMBL152145 — IC50 = 8.71 nM 8.06
CHEMBL154931 — IC50 = 9.0 nM 8.05
CHEMBL443559 — IC50 = 9.099 nM 8.04
CHEMBL443559 — IC50 = 9.1 nM 8.04
CHEMBL154931 — IC50 = 9.016 nM 8.04
CHEMBL153045 — IC50 = 9.311 nM 8.03
CHEMBL153045 — IC50 = 9.3 nM 8.03
CHEMBL153384 — IC50 = 10.0 nM 8.00
CHEMBL422149 — IC50 = 9.9 nM 8.00
CHEMBL153384 — IC50 = 10.0 nM 8.00
CHEMBL422149 — IC50 = 9.908 nM 8.00
CHEMBL2283572 — IC50 = 12.02 nM 7.92
CHEMBL2283572 — IC50 = 12.0 nM 7.92
CHEMBL2283573 — IC50 = 13.0 nM 7.89
CHEMBL2283574 — IC50 = 18.0 nM 7.75
CHEMBL2283574 — IC50 = 18.03 nM 7.74
CHEMBL153457 — IC50 = 19.01 nM 7.72
CHEMBL153457 — IC50 = 19.0 nM 7.72
CHEMBL2283573 — IC50 = 30.06 nM 7.52
CHEMBL151856 — IC50 = 55.08 nM 7.26
CHEMBL151856 — IC50 = 55.0 nM 7.26
CHEMBL433543 — IC50 = 65.01 nM 7.19
CHEMBL433543 — IC50 = 65.0 nM 7.19
CHEMBL358236 — IC50 = 70.0 nM 7.16
CHEMBL358236 — IC50 = 70.15 nM 7.15
CHEMBL2283472 — IC50 = 74.0 nM 7.13
CHEMBL435640 — IC50 = 74.0 nM 7.13
CHEMBL435640 — IC50 = 74.13 nM 7.13
CHEMBL2283472 — IC50 = 74.13 nM 7.13
CHEMBL358445 — IC50 = 78.0 nM 7.11
CHEMBL358445 — IC50 = 79.07 nM 7.10
CHEMBL358396 — IC50 = 94.0 nM 7.03
CHEMBL358396 — IC50 = 94.19 nM 7.03