cyproheptadine


SMILES CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1
InChIKey JJCFRYNCJDLXIK-UHFFFAOYSA-N

Chemical properties

Hydrogen bond acceptors 1
Hydrogen bond donors 0
Rotatable bonds 0
Molecular weight (Da) 287.2

Drug properties

Molecular type Small molecule
Physiological/Surrogate Surrogate
Approved drug Yes

Database connections

Ligand site mutations 5-HT2A 5-HT2C

Bioactivities

Receptor Activity Source
GTP Uniprot Species Family Class Type Min Avg Max Database
5-HT6 5HT6R Human 5-Hydroxytryptamine A pKi 6.8 6.8 6.8 Guide to Pharmacology
5-HT7 5HT7R Human 5-Hydroxytryptamine A pKi 6.9 6.9 6.9 Guide to Pharmacology
α1A ADA1A Human Adrenoceptors A pKi 7.4 7.4 7.4 Guide to Pharmacology
α1B ADA1B Human Adrenoceptors A pKi 7.6 7.6 7.6 Guide to Pharmacology
α1D ADA1D Human Adrenoceptors A pKi 6.9 6.9 6.9 Guide to Pharmacology
5-HT6 5HT6R Rat 5-Hydroxytryptamine A pKi 6.9 6.9 6.9 Guide to Pharmacology
5-HT7 5HT7R Rat 5-Hydroxytryptamine A pKi 7.1 7.3 7.5 Guide to Pharmacology
D2 DRD2 Mouse Dopamine A pKi 6.95 6.95 6.95 ChEMBL
5-HT7 5HT7R Rat 5-Hydroxytryptamine A pKi 7.3 7.3 7.3 ChEMBL
5-HT1B 5HT1B Rat 5-Hydroxytryptamine A pKi 5.9 5.9 5.9 ChEMBL
α1B ADA1B Rat Adrenoceptors A pKi 7.36 7.36 7.36 ChEMBL
α1A ADA1A Rat Adrenoceptors A pKi 7.01 7.01 7.01 ChEMBL
α1D ADA1D Human Adrenoceptors A pKi 7.28 7.28 7.28 ChEMBL
α2B ADA2B Human Adrenoceptors A pKi 7.77 7.77 7.77 ChEMBL
M5 ACM5 Human Acetylcholine (muscarinic) A pKi 8.56 8.56 8.56 ChEMBL
α2C ADA2C Human Adrenoceptors A pKi 6.73 6.73 6.73 ChEMBL
H2 HRH2 Human Histamine A pKi 6.71 6.71 6.71 ChEMBL
5-HT7 5HT7R Human 5-Hydroxytryptamine A pKi 6.9 7.1 7.3 ChEMBL
M4 ACM4 Human Acetylcholine (muscarinic) A pKi 8.66 8.66 8.66 ChEMBL
H1 HRH1 Human Histamine A pKd 5.27 5.27 5.27 ChEMBL
H1 HRH1 Human Histamine A pKi 9.37 9.37 9.37 ChEMBL
M3 ACM3 Human Acetylcholine (muscarinic) A pKi 8.02 8.02 8.02 ChEMBL
5-HT1A 5HT1A Rat 5-Hydroxytryptamine A pKi 7.16 7.16 7.16 ChEMBL
α2A ADA2A Human Adrenoceptors A pKi 6.97 6.97 6.97 ChEMBL
D1 DRD1 Human Dopamine A pKi 7.1 7.1 7.1 ChEMBL
5-HT6 5HT6R Human 5-Hydroxytryptamine A pKi 6.89 6.89 6.89 ChEMBL
5-HT2B 5HT2B Human 5-Hydroxytryptamine A pKi 8.22 8.22 8.22 ChEMBL
M2 ACM2 Human Acetylcholine (muscarinic) A pKi 7.92 7.92 7.92 ChEMBL
5-HT2C 5HT2C Human 5-Hydroxytryptamine A pKi 7.96 8.43 8.89 ChEMBL
M1 ACM1 Human Acetylcholine (muscarinic) A pKi 8.4 8.4 8.4 ChEMBL
D3 DRD3 Human Dopamine A pKi 7.8 7.8 7.8 ChEMBL
5-HT2A 5HT2A Human 5-Hydroxytryptamine A pKi 8.52 9.05 9.56 ChEMBL
5-HT2C K7GSR7 Pig 5-Hydroxytryptamine A pKi 7.86 7.95 8.08 PDSP Ki database
D2 DRD2 Human Dopamine A pKi 6.95 7.11 7.26 ChEMBL
5-HT1B 5HT1B Rat 5-Hydroxytryptamine A pKi 5.32 5.57 6.08 PDSP Ki database
5-HT1D 5HT1D Human 5-Hydroxytryptamine A pKi 5.89 6.03 6.17 PDSP Ki database
5-HT1D F1MMU1 Bovine 5-Hydroxytryptamine A pKi 5.92 5.92 5.92 PDSP Ki database
α1B ADA1B Human Adrenoceptors A pKi 8.12 8.12 8.12 Drug Central
5-HT2A 5HT2A Human 5-Hydroxytryptamine A pKi 7.59 8.49 9.34 PDSP Ki database
5-HT2A 5HT2A Rat 5-Hydroxytryptamine A pKi 7.81 8.72 9.36 PDSP Ki database
5-HT2A 5HT2A Bovine 5-Hydroxytryptamine A pKi 8.52 8.52 8.52 PDSP Ki database
D1 DRD1 Human Dopamine A pKi 6.93 7.46 8.0 PDSP Ki database
D2 DRD2 Human Dopamine A pKi 6.95 7.04 7.13 PDSP Ki database
D3 DRD3 Human Dopamine A pKi 8.1 8.1 8.1 PDSP Ki database
5-HT1A 5HT1A Human 5-Hydroxytryptamine A pKi 7.0 7.21 7.3 PDSP Ki database
5-HT2C 5HT2C Rat 5-Hydroxytryptamine A pKi 7.55 7.84 8.2 PDSP Ki database
5-HT6 5HT6R Rat 5-Hydroxytryptamine A pKi 6.87 6.87 6.87 PDSP Ki database
5-HT6 5HT6R Human 5-Hydroxytryptamine A pKi 6.82 6.9 7.02 PDSP Ki database
5-HT7 5HT7R Rat 5-Hydroxytryptamine A pKi 7.11 7.3 7.47 PDSP Ki database
5-HT2B 5HT2B Human 5-Hydroxytryptamine A pKi 8.59 8.7 8.81 PDSP Ki database
5-HT2C 5HT2C Human 5-Hydroxytryptamine A pKi 7.74 8.2 8.65 PDSP Ki database
5-HT7 5HT7R Guinea pig 5-Hydroxytryptamine A pKi 6.3 6.6 6.9 PDSP Ki database
5-HT7 5HT7R Human 5-Hydroxytryptamine A pKi 6.91 7.11 7.52 PDSP Ki database
H1 HRH1 Human Histamine A pKi 10.22 10.22 10.22 PDSP Ki database
H1 HRH1 Guinea pig Histamine A pKi 10.0 10.0 10.0 PDSP Ki database
H1 HRH1 Rat Histamine A pKi 8.51 8.51 8.51 PDSP Ki database
H3 HRH3 Human Histamine A pKi 5.0 5.0 5.0 PDSP Ki database
H4 HRH4 Human Histamine A pKi 5.0 5.85 6.7 PDSP Ki database
5-HT2B 5HT2B Mouse 5-Hydroxytryptamine A pKi 7.65 7.65 7.65 PDSP Ki database
5-HT1A 5HT1A Rat 5-Hydroxytryptamine A pKi 5.28 6.26 6.96 PDSP Ki database
D2 DRD2 Bovine Dopamine A pKi 7.19 7.19 7.19 PDSP Ki database
D1 DRD1 Bovine Dopamine A pKi 5.92 5.92 5.92 PDSP Ki database
D2 DRD2 Rat Dopamine A pKi 6.95 6.95 6.95 PDSP Ki database
M1 ACM1 Human Acetylcholine (muscarinic) A pKi 7.72 7.82 7.92 PDSP Ki database
M3 ACM3 Human Acetylcholine (muscarinic) A pKi 7.92 7.92 7.92 PDSP Ki database
M4 ACM4 Human Acetylcholine (muscarinic) A pKi 7.72 7.91 8.1 PDSP Ki database
M5 ACM5 Human Acetylcholine (muscarinic) A pKi 7.93 8.14 8.35 PDSP Ki database
5-HT1B 5HT1B Human 5-Hydroxytryptamine A pKi 5.8 5.8 5.8 PDSP Ki database
5-HT5A 5HT5A Human 5-Hydroxytryptamine A pKi 7.24 7.24 7.24 PDSP Ki database
M2 ACM2 Human Acetylcholine (muscarinic) A pKi 7.74 7.95 8.15 PDSP Ki database
D4 DRD4 Human Dopamine A pKi 6.92 6.92 6.92 PDSP Ki database
D5 DRD5 Human Dopamine A pKi 7.22 7.22 7.22 PDSP Ki database
5-HT1A 5HT1A Human 5-Hydroxytryptamine A pKi 8.14 8.14 8.14 Drug Central
5-HT1D 5HT1D Human 5-Hydroxytryptamine A pKi 8.23 8.23 8.23 Drug Central
5-HT2A 5HT2A Human 5-Hydroxytryptamine A pKi 8.07 8.07 8.07 Drug Central
5-HT2B 5HT2B Human 5-Hydroxytryptamine A pKi 8.05 8.05 8.05 Drug Central
5-HT2C 5HT2C Human 5-Hydroxytryptamine A pKi 8.06 8.06 8.06 Drug Central
5-HT6 5HT6R Human 5-Hydroxytryptamine A pKi 8.17 8.17 8.17 Drug Central
5-HT7 5HT7R Human 5-Hydroxytryptamine A pKi 8.16 8.16 8.16 Drug Central
M1 ACM1 Human Acetylcholine (muscarinic) A pKi 8.1 8.1 8.1 Drug Central
M2 ACM2 Human Acetylcholine (muscarinic) A pKi 8.1 8.1 8.1 Drug Central
M3 ACM3 Human Acetylcholine (muscarinic) A pKi 8.1 8.1 8.1 Drug Central
M5 ACM5 Human Acetylcholine (muscarinic) A pKi 8.07 8.07 8.07 Drug Central
α1A ADA1A Human Adrenoceptors A pKi 8.13 8.13 8.13 Drug Central
α1D ADA1D Human Adrenoceptors A pKi 8.16 8.16 8.16 Drug Central
α2A ADA2A Human Adrenoceptors A pKi 8.16 8.16 8.16 Drug Central
α2B ADA2B Human Adrenoceptors A pKi 8.11 8.11 8.11 Drug Central
α2C ADA2C Human Adrenoceptors A pKi 8.17 8.17 8.17 Drug Central
D1 DRD1 Human Dopamine A pKi 8.16 8.16 8.16 Drug Central
D2 DRD2 Human Dopamine A pKi 8.16 8.16 8.16 Drug Central
D3 DRD3 Human Dopamine A pKi 8.09 8.09 8.09 Drug Central
H1 HRH1 Human Histamine A pKi 7.99 7.99 7.99 Drug Central
H4 HRH4 Human Histamine A pKi 8.09 8.09 8.09 Drug Central
5-HT6 5HT6R Rat 5-Hydroxytryptamine A pKi 8.16 8.16 8.16 Drug Central
5-HT2A 5HT2A Rat 5-Hydroxytryptamine A pKi 8.06 8.06 8.06 Drug Central
α1B ADA1B Rat Adrenoceptors A pKi 8.13 8.13 8.13 Drug Central
H1 HRH1 Guinea pig Histamine A pKd 8.05 8.05 8.05 Drug Central
5-HT1B 5HT1B Rat 5-Hydroxytryptamine A pKi 8.23 8.23 8.23 Drug Central
5-HT7 5HT7R Rat 5-Hydroxytryptamine A pKi 8.14 8.14 8.14 Drug Central
5-HT2C 5HT2C Mouse 5-Hydroxytryptamine A pKi 8.1 8.1 8.1 Drug Central
5-HT1A A0A4X1UTF5 Pig 5-Hydroxytryptamine A pKi 6.45 6.45 6.45 PDSP Ki database
M4 ACM4 Human Acetylcholine (muscarinic) A pKi 8.06 8.06 8.06 Drug Central
H1 HRH1 Human Histamine A pKi 10.2 10.2 10.2 Guide to Pharmacology
H2 HRH2 Human Histamine A pKi 8.17 8.17 8.17 Drug Central
D2 DRD2 Mouse Dopamine A pKi 8.16 8.16 8.16 Drug Central
H1 HRH1 Guinea pig Histamine A pKd 9.0 9.0 9.0 ChEMBL
H1 HRH1 Guinea pig Histamine A pKi 9.27 9.27 9.27 ChEMBL
5-HT2C 5HT2C Mouse 5-Hydroxytryptamine A pKi 7.96 7.96 7.96 ChEMBL
Receptor Activity Source
GTP Uniprot Species Family Class Type Min Avg Max Database
5-HT1B 5HT1B Rat 5-Hydroxytryptamine A pIC50 5.56 5.56 5.56 ChEMBL
α1B ADA1B Rat Adrenoceptors A pIC50 7.1 7.1 7.1 ChEMBL
α1A ADA1A Rat Adrenoceptors A pIC50 6.62 6.62 6.62 ChEMBL
M1 ACM1 Rat Acetylcholine (muscarinic) A Potency 7.5 7.58 7.65 ChEMBL
α1D ADA1D Human Adrenoceptors A pIC50 6.97 6.97 6.97 ChEMBL
α2B ADA2B Human Adrenoceptors A pIC50 7.42 7.42 7.42 ChEMBL
M5 ACM5 Human Acetylcholine (muscarinic) A pIC50 8.42 8.42 8.42 ChEMBL
α2C ADA2C Human Adrenoceptors A pIC50 5.89 5.89 5.89 ChEMBL
H2 HRH2 Human Histamine A pIC50 6.7 6.7 6.7 ChEMBL
M4 ACM4 Human Acetylcholine (muscarinic) A pIC50 7.8 7.8 7.8 ChEMBL
H1 HRH1 Human Histamine A pIC50 8.43 8.43 8.43 ChEMBL
M3 ACM3 Human Acetylcholine (muscarinic) A pIC50 7.34 7.34 7.34 ChEMBL
D2 DRD2 Rat Dopamine A pIC50 6.85 6.85 6.85 ChEMBL
5-HT1A 5HT1A Rat 5-Hydroxytryptamine A pIC50 6.91 6.91 6.91 ChEMBL
α2A ADA2A Human Adrenoceptors A pIC50 6.55 6.55 6.55 ChEMBL
D1 DRD1 Human Dopamine A pIC50 6.8 6.8 6.8 ChEMBL
5-HT6 5HT6R Human 5-Hydroxytryptamine A pIC50 6.55 6.55 6.55 ChEMBL
5-HT2B 5HT2B Human 5-Hydroxytryptamine A pIC50 8.03 8.03 8.03 ChEMBL
M2 ACM2 Human Acetylcholine (muscarinic) A pIC50 7.46 7.46 7.46 ChEMBL
5-HT2C 5HT2C Human 5-Hydroxytryptamine A pIC50 8.61 8.61 8.61 ChEMBL
M1 ACM1 Human Acetylcholine (muscarinic) A pIC50 7.8 7.8 7.8 ChEMBL
D3 DRD3 Human Dopamine A pIC50 7.32 7.32 7.32 ChEMBL
5-HT2A 5HT2A Human 5-Hydroxytryptamine A pIC50 9.01 9.01 9.01 ChEMBL
D2 DRD2 Human Dopamine A pIC50 6.79 6.79 6.79 ChEMBL
TSH TSHR Human Glycoprotein hormone A Potency 5.0 5.33 6.0 ChEMBL
5-HT1A 5HT1A Rat 5-Hydroxytryptamine A pIC50 8.16 8.16 8.16 Drug Central
α1A ADA1A Rat Adrenoceptors A pIC50 8.18 8.18 8.18 Drug Central
D2 DRD2 Rat Dopamine A pIC50 8.16 8.16 8.16 Drug Central